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Keywords = hypromellose

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13 pages, 1103 KiB  
Article
Prolonged Gel Delivery to Oral Cavity from a Silicone Tube: In Vivo Assessment
by Suhail Alghanem, Ewelina Dziurkowska, Mateusz Lampkowski, Iwona Ordyniec-Kwaśnica and Małgorzata Sznitowska
Pharmaceutics 2025, 17(9), 1095; https://doi.org/10.3390/pharmaceutics17091095 - 22 Aug 2025
Abstract
Objectives: This study evaluated the comfort of using silicone tubes installed in the oral cavity as a reservoir for a hydrogel that allows for a slow delivery of the active substance acting locally or systemically. Methods: Perforated silicone tubes 8 cm [...] Read more.
Objectives: This study evaluated the comfort of using silicone tubes installed in the oral cavity as a reservoir for a hydrogel that allows for a slow delivery of the active substance acting locally or systemically. Methods: Perforated silicone tubes 8 cm long with two internal diameters were used: T1 (1.5 mm) and T2 (2.4 mm). The reservoirs were filled with hydrogel placebo formulations: carbomer 1.5% (C), hydroxyethylcellulose 4% (HEC), or hydroxypropylmethylcellulose (hypromellose) 3% (HPMC). Physical parameters of the gel were determined with a viscometer and a texture analyzer. During 4 h of application, the volunteers reported sensory perceptions, and the rate of gel erosion was evaluated. The results were correlated with the viscosity, rheology, and dissolution rate of the gels measured in vitro. Results: Volunteers reported only mild discomfort wearing the device, preferring smaller-sized tubes. The tubes were easy to apply and generally comfortable, with no reports of significant discomfort. Despite similar viscosity and rheology, the polymer type had a significant impact on erosion rate, both in vitro and in vivo. After 4 h of application in vivo, more than 90% of the carbomer gel remained in the tube, while in the case of less cohesive HPMC or HEC gels, this was about 50%. A statistically significant correlation was observed between the in vitro and in vivo mean erosion percentages for the HEC and HPMC gels. Conclusions: This study supports the use of silicone tubes as effective reservoir devices for prolonging the residence time of drug formulations in the oral cavity. Full article
(This article belongs to the Special Issue Development and Optimization of Buccal Films Formulations)
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27 pages, 27757 KiB  
Article
Continuous Processing Strategies for Amorphous Solid Dispersions of Itraconazole: Impact of Polymer Selection and Manufacturing Techniques
by Madhuri M. Kshirsagar, Bandoo C. Chatale, Sathish Dyawanapelly, Lalitkumar K. Vora and Purnima D. Amin
Pharmaceutics 2025, 17(9), 1090; https://doi.org/10.3390/pharmaceutics17091090 - 22 Aug 2025
Viewed by 44
Abstract
Background: The limited aqueous solubility of BCS Class II drugs, exemplified by itraconazole (ITR), continues to hinder their bioavailability and therapeutic performance following oral administration. The present study investigated the development of amorphous solid dispersions (ASDs) of ITR via continuous manufacturing technologies, [...] Read more.
Background: The limited aqueous solubility of BCS Class II drugs, exemplified by itraconazole (ITR), continues to hinder their bioavailability and therapeutic performance following oral administration. The present study investigated the development of amorphous solid dispersions (ASDs) of ITR via continuous manufacturing technologies, such as hot melt extrusion (HME) and spray drying (SD), to improve drug release. Methods: Polymer selection was guided by Hansen solubility parameter (HSP) analysis, film casting, and molecular modeling, leading to the identification of aminoalkyl methacrylate copolymer type A (Eudragit® EPO), polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus®), and hypromellose acetate succinate HG (AQOAT® AS-HG) as suitable carriers. ASDs were prepared at drug-to-polymer ratios of 1:1, 1:2, and 2:1. Comprehensive characterization was performed using ATR-FTIR, NMR, DSC, PXRD, SEM, PLM, and contact angle analysis. Results: HME demonstrated higher process efficiency, solvent-free operation, and superior dissolution enhancement compared to SD. Optimized HME-based ASDs were formulated into tablets. The ITR–Eudragit® EPO formulation achieved 95.88% drug release within 2 h (Weibull model, R2 > 0.99), while Soluplus® and AQOAT® AS-HG systems achieved complete release, best described by the Peppas–Sahlin model. Molecular modeling confirmed favorable drug–polymer interactions, correlating with the formation of stable complex and enhanced release performance. Conclusions: HME-based continuous manufacturing provides a scalable and robust strategy for improving the oral delivery of poorly water-soluble drugs. Integrating predictive modeling with experimental screening enables the rational design of ASD formulations with optimized dissolution behavior, offering potential for improved therapeutic outcomes in BCS Class II drug delivery. Full article
(This article belongs to the Special Issue Advances in Hot Melt Extrusion Technology)
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30 pages, 933 KiB  
Review
Hydroxypropyl Methylcellulose—A Key Excipient in Pharmaceutical Drug Delivery Systems
by Robert-Alexandru Vlad, Andrada Pintea, Cezara Pintea, Emőke-Margit Rédai, Paula Antonoaea, Magdalena Bîrsan and Adriana Ciurba
Pharmaceutics 2025, 17(6), 784; https://doi.org/10.3390/pharmaceutics17060784 - 16 Jun 2025
Cited by 1 | Viewed by 3745
Abstract
Hydroxypropyl methylcellulose (Hypromellose, HPMC) is a well-known excipient used in the pharmaceutical and nutraceutical fields due to its versatile physicochemical properties. HPMC (derived from cellulose and obtained through etherification) varies in polymerization degree and viscosity, factors that both influence its functional applications. Usually, [...] Read more.
Hydroxypropyl methylcellulose (Hypromellose, HPMC) is a well-known excipient used in the pharmaceutical and nutraceutical fields due to its versatile physicochemical properties. HPMC (derived from cellulose and obtained through etherification) varies in polymerization degree and viscosity, factors that both influence its functional applications. Usually, an increased polymerization degree implies a higher viscosity, depending also on the amount of polymer used. Hypromellose plays a crucial role in solid dosage forms, serving as a binder in the case of controlled-release tablets, a film-forming agent in the case of orodispersible films and mucoadhesive films, and a release modifier due to its presence in different polymerization degrees in the case of extended or modified release tablets. However, its compatibility with other excipients and the active ingredient must be carefully evaluated to prevent formulation challenges via several analytical methods such as differential scanned calorimetry (DSC), Fourier Transformed Infrared spectroscopy (FT-IR), X-Ray Particle Diffraction (XRPD), and Scanning Electron Microscopy (SEM). This review explores the physicochemical characteristics, and diverse applications of HPMC, emphasizing its significance in modern drug delivery systems. Full article
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28 pages, 6539 KiB  
Article
Hydrogel–Nanolipid Formulations for the Complex Anti-Inflammatory and Antimicrobial Therapy of Periodontitis
by Rabia Ashfaq, Nóra Tóth, Anita Kovács, Szilvia Berkó, Gábor Katona, Rita Ambrus, Tamás Ferenc Polgár, Mária Szécsényi, Katalin Burián and Mária Budai-Szűcs
Pharmaceutics 2025, 17(5), 620; https://doi.org/10.3390/pharmaceutics17050620 - 7 May 2025
Viewed by 869
Abstract
Objectives: This study aimed to develop and evaluate nanostructured lipid carriers (NLCs) loaded with meloxicam (Melox) and a therapeutic antibacterial and anti-inflammatory liquid lipid, clove oil (CO) for periodontitis treatment, a complex inflammatory condition necessitating advanced drug delivery systems. The NLC–Melox formulation [...] Read more.
Objectives: This study aimed to develop and evaluate nanostructured lipid carriers (NLCs) loaded with meloxicam (Melox) and a therapeutic antibacterial and anti-inflammatory liquid lipid, clove oil (CO) for periodontitis treatment, a complex inflammatory condition necessitating advanced drug delivery systems. The NLC–Melox formulation was integrated into three hydrogels, hypromellose (HPMC), zinc hyaluronate (ZnHA), and sodium hyaluronate (NaHA), to conduct a comparative analysis focusing on enhanced localized drug delivery, improved mucoadhesion, prolonged retention, and significant therapeutic outcomes. Methods: NLC–Melox was prepared by homogenization and characterized by dynamic light scattering (DLS). Subsequently, NLC–Melox-loaded gels were subjected to transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), Raman spectroscopy, and rheological analysis. In vitro drug release, anti-inflammatory activity (BSA denaturation assay), and antibacterial efficacy (MIC, MBC) were investigated to assess therapeutic potential. Results: DLS revealed a particle size of 183 nm with a polydispersity index of 0.26, indicating homogeneity. TEM confirmed consistent morphology and uniform nanoparticle distribution. DSC and XRD demonstrated the amorphous nature of Melox, enhancing solubility and stability. Spectroscopy confirmed no chemical interactions between components. Rheological studies identified ZnHA as the most mucoadhesive and structurally stable gel. In vitro release studies showed sustained drug release over 24 h. Melox and CO-loaded formulations demonstrated significant anti-inflammatory activity and notable antibacterial efficacy due to the antibacterial oil. Conclusions: The study highlighted the potential of NLC-based mucoadhesive hydrogels as an effective strategy for periodontitis treatment. The formulation offered improved drug solubility, therapeutic efficacy, mucoadhesivity, and prolonged delivery, making it a promising candidate for localized therapy. Full article
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30 pages, 4026 KiB  
Article
Film-Forming Microemulsions with Essential Oils: Elucidating Relationships Between Formulation Parameters, Thermodynamic Stability, and Quality Attributes
by Ljiljana Đekić, Ana Ćirić, Sandra Milinković, Jelena Milinković Budinčić, Jadranka Fraj and Lidija Petrović
Processes 2025, 13(4), 990; https://doi.org/10.3390/pr13040990 - 26 Mar 2025
Viewed by 1067
Abstract
The incorporation of essential oils into the oil phase of oil-in-water microemulsions is an emerging strategy for the development of stable water-based topical formulations. The introduction of a suitable polymer to formulate film-forming microemulsions may improve topical administration; however, the effect of formulation [...] Read more.
The incorporation of essential oils into the oil phase of oil-in-water microemulsions is an emerging strategy for the development of stable water-based topical formulations. The introduction of a suitable polymer to formulate film-forming microemulsions may improve topical administration; however, the effect of formulation variables on film quality attributes has not been studied. In this study, thermodynamically stable microemulsion concentrates consisting of surfactant (Kolliphor® RH40), alone or in combination with cosurfactant Transcutol® at surfactant-to-cosurfactant mass ratio 7:3, cosolvent (propylene glycol), and synthetic oils (medium-chain triglycerides or isopropyl myristate) with tea tree, cinnamon, or thyme essential oil were formulated and diluted with hypromellose solution in a water/isopropanol mixture (1:1 w/w) to produce film-forming microemulsions. The type and concentration of synthetic and essential oils and cosurfactant influenced the dynamics of structural transformations upon dilution as well as the rheological behavior, viscosity, and pH of film-forming microemulsions. Films obtained by casting film-forming microemulsions were opalescent, smooth, flexible, and swellable in artificial sweat and water. The weight and yield of films increase with the synthetic oils present and without cosurfactant added. Optimizing the ratio of essential oil/synthetic oil, the type of synthetic oil, and the inclusion/exclusion of cosurfactant allows for achieving the targeted film attributes for cosmetic and pharmaceutical applications, including wound treatment. Full article
(This article belongs to the Special Issue Advances in Interactions of Polymers in Emulsion Systems)
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19 pages, 1286 KiB  
Review
Hydrogel Delivery Systems for Biological Active Substances: Properties and the Role of HPMC as a Carrier
by Arailym Amanzholkyzy, Shynar Zhumagaliyeva, Nurgul Sultanova, Zharylkasyn Abilov, Damira Ongalbek, Elvira Donbayeva, Aktoty Niyazbekova and Zhazira Mukazhanova
Molecules 2025, 30(6), 1354; https://doi.org/10.3390/molecules30061354 - 18 Mar 2025
Cited by 2 | Viewed by 2652
Abstract
Hydrogel delivery systems are popular dosage forms that have a number of advantages, such as ease of use, painlessness, increased efficiency due to prolongation of rheological, swelling and sorption characteristics, regulation of drug release, and stimulus sensitivity. Particular interest is shown in hydrogels [...] Read more.
Hydrogel delivery systems are popular dosage forms that have a number of advantages, such as ease of use, painlessness, increased efficiency due to prolongation of rheological, swelling and sorption characteristics, regulation of drug release, and stimulus sensitivity. Particular interest is shown in hydrogels of cellulose ether derivatives due to the possibility of obtaining their modified forms to vary the solubility, the degree of prolonged action, and the release of the active substance, as well as their widespread availability, affordability, and the possibility of sourcing raw materials from different sources. Hydroxypropyl methylcellulose (HPMC, “hypromellose”) is one of the most popular cellulose ethers in the production of medicines as a filler, coating and carrier. Research on hydrogel carriers based on polymer complexes and modified forms of HPMC using acrylic, citric, and lactic acids, PVP, chitosan, Na-CMC, and gelatin is of particular interest, as they provide the necessary rheological and swelling characteristics. There is growing interest in medical transdermal hydrogels, films, capsules, membranes, nanocrystals, and nanofibers based on HPMC with the incorporation of biologically active substances (BASs), especially those of plant origin, as antibacterial, wound-healing, antimicrobial, mucoadhesive, anti-inflammatory, and antioxidant agents. The aim of this article is to review modern research and achievements in the field of hydrogel systems based on cellulose ethers, particularly HPMC, analyzing their properties, methods of production, and prospects for application in medicine and pharmacy. Full article
(This article belongs to the Section Macromolecular Chemistry)
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24 pages, 5579 KiB  
Article
Uptake and Inhibition of P-Glycoprotein-Mediated Efflux Evaluation of Encapsulated Methotrexate Chitosan and Hypromellose Phthalate Nanoparticles for Potential Glioblastoma Treatment
by Valéria de Moura Leite Naves, Rafaela Franco Dias Bruzadelli, Marisa Ionta, Maria Palmira Daflon Gremião, Liliane Neves Pedreiro, Gislaine Ribeiro Pereira and Flávia Chiva Carvalho
Pharmaceutics 2025, 17(2), 239; https://doi.org/10.3390/pharmaceutics17020239 - 12 Feb 2025
Cited by 2 | Viewed by 1015
Abstract
Background: Methotrexate (MTX), a folic acid antagonist used in chemotherapy, faces limitations due to cancer cell resistance, high toxicity, and low bioavailability. Objective: This study developed nanoparticles (NPs) of chitosan (QS) and hydroxypropylmethylcellulose phthalate (HPMCP) to encapsulate MTX for potential effect investigation on [...] Read more.
Background: Methotrexate (MTX), a folic acid antagonist used in chemotherapy, faces limitations due to cancer cell resistance, high toxicity, and low bioavailability. Objective: This study developed nanoparticles (NPs) of chitosan (QS) and hydroxypropylmethylcellulose phthalate (HPMCP) to encapsulate MTX for potential effect investigation on glioblastoma cell targeting and P-gp efflux inhibition. Method: NPs were produced by the polyelectrolyte complexation method and were characterized by DLS, PDI, DSC, FTIR, PXRD, MEV, drug release profile, and an in vitro mucoadhesion test. Cell viability, flow cytometry, and LSCM using U251MG (glioblastoma) and CCD 1059Sk (fibroblasts) cells were used to evaluate glioblastoma and the P-gp efflux effect. Results: NPPM29 (QS3:1) showed 91.72% encapsulation efficiency, a mean diameter of 452.6 nm, and a zeta potential of +22.5 mV. DSC, FTIR, and PXRD confirmed the QS-HPMCP supramolecular interaction. Liquid falling mucoadhesion tests demonstrated strong retention of NPPM29 (84%) compared to free MTX (10.5%). In vitro release studies indicated controlled drug release at pH 7.4. Cytotoxicity assays in U251MG revealed enhanced efficacy of NPPM29 (IC50 = 68.79 µg/mL) compared to free MTX (IC50 = 80.54 µg/mL), with minimal impact on fibroblasts, confirming tumor specificity. Flow cytometry and LSCM confirmed improved cellular internalization and P-gp inhibition. Conclusions: These findings highlight the potential of MTX-QS-HPMCP-NPs for glioblastoma therapy. Full article
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16 pages, 5027 KiB  
Article
Evaluation of Drug–Polymer and Drug–Drug Interaction in Cellulosic Multi-Drug Delivery Matrices
by Abdullah Isreb, Mohamed A. Alhnan, Abdulrahman Mkia, Khaled Al-Jammal, Abdallah Yaghi, Enoche Florence Oga, Peter Timmins, Michael Bonner and Robert T. Forbes
Methods Protoc. 2025, 8(1), 4; https://doi.org/10.3390/mps8010004 - 6 Jan 2025
Cited by 1 | Viewed by 1302
Abstract
Multi-drug delivery systems have gained increasing interest from the pharmaceutical industry. Alongside this is the interest in amorphous solid dispersions as an approach to achieve effective oral delivery of compounds with solubility-limited bioavailability. Despite this, there is limited information regarding predicting the behavior [...] Read more.
Multi-drug delivery systems have gained increasing interest from the pharmaceutical industry. Alongside this is the interest in amorphous solid dispersions as an approach to achieve effective oral delivery of compounds with solubility-limited bioavailability. Despite this, there is limited information regarding predicting the behavior of two or more drugs (in amorphous forms) in a polymeric carrier and whether molecular interactions between the compounds, between each compound, and if the polymer have any effect on the physical properties of the system. This work studies the interaction between model drug combinations (two of ibuprofen, malonic acid, flurbiprofen, or naproxen) dispersed in a polymeric matrix of hypromellose acetate succinate (HPMCAS) using a solvent evaporation technique. Hildebrand and Hansen calculations were used to predict the miscibility of compounds as long as the difference in their solubility parameter values was not greater than 7 MPa1/2. It was observed that the selected APIs (malonic acid, ibuprofen, naproxen, and flurbiprofen) were miscible within the formed polymeric matrix. Adding the API caused depression in the Tg of the polymer to certain concentrations (17%, 23%, 13%) for polymeric matrices loaded with malonic acid, ibuprofen, and naproxen, respectively. Above this, large crystals started to form, and phase separation was seen. Adding two APIs to the same matrix resulted in reducing the saturation concentration of one of the APIs. A trend was observed and linked to Hildebrand and Hansen solubility parameters (HSP). Full article
(This article belongs to the Special Issue Feature Papers in Methods and Protocols 2024)
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17 pages, 6287 KiB  
Article
A Quaternary Solid Dispersion System for Improving the Solubility of Olaparib
by Tae-Han Yun, Jeong-Gyun Lee, Kyu-Ho Bang, Jung-Hyun Cho and Kyeong-Soo Kim
Solids 2025, 6(1), 1; https://doi.org/10.3390/solids6010001 - 2 Jan 2025
Cited by 1 | Viewed by 2117
Abstract
To improve the low solubility of poorly water soluble olaparib, in the following study, we prepared olaparib-loaded quaternary solid dispersions with hypromellose, Tween 20 or Labrasol, and colloidal silica. The solubility of olaparib with various types of surfactants was evaluated to select the [...] Read more.
To improve the low solubility of poorly water soluble olaparib, in the following study, we prepared olaparib-loaded quaternary solid dispersions with hypromellose, Tween 20 or Labrasol, and colloidal silica. The solubility of olaparib with various types of surfactants was evaluated to select the most suitable surfactant to effectively enhance its solubility, and subsequently, olaparib-loaded quaternary solid dispersions were prepared through spray drying. The physicochemical properties of the prepared olaparib-loaded quaternary solid dispersions were investigated using scanning electron microscopy, flowability, powder X-ray diffraction, and Fourier-transform infrared spectroscopy. The particle size of the olaparib-loaded quaternary solid dispersions was smaller and more spherical compared to the olaparib drug powder and maintained an amorphous state, and olaparib exhibited no intermolecular interactions with other excipients within the solid dispersion. Additionally, they exhibited enhanced flow properties compared to the olaparib drug powder. The results of subsequent kinetic solubility tests and dissolution tests demonstrated that the surfactant influenced the enhancement of the solubility and drug release of olaparib. Therefore, olaparib-loaded quaternary solid dispersions, characterized by enhanced solubility, will be beneficial for the oral delivery of poorly soluble olaparib. Full article
(This article belongs to the Special Issue Amorphous Materials: Fabrication, Properties, and Applications)
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12 pages, 9039 KiB  
Article
Phase Separation Investigation of Axitinib in Supersaturated Solution
by Jie Xu, Jianshuo Su, Huaizhen Zhang, Rupeng Bu, Zhuang Ding, Ning Zhang and Yanna Zhao
Crystals 2024, 14(12), 1042; https://doi.org/10.3390/cryst14121042 - 30 Nov 2024
Viewed by 947
Abstract
Phase separation is quite common in formulations for hydrophobic active pharmaceutical ingredients (APIs) due to their thermodynamic instability in a supersaturated state during in vitro dissolution or in vivo absorption. Phase separation possibly accompanies the formation of a disordered drug-rich phase, but this [...] Read more.
Phase separation is quite common in formulations for hydrophobic active pharmaceutical ingredients (APIs) due to their thermodynamic instability in a supersaturated state during in vitro dissolution or in vivo absorption. Phase separation possibly accompanies the formation of a disordered drug-rich phase, but this is still not thoroughly understood. In this study, the phase separation of supersaturated axitinib (Axi) in media with or without polymers was evaluated via multiple analytical methods, including UV–vis and fluorescence spectroscopy, dynamic light scattering, and microscopy. The phase separation of Axi occurred at an Axi concentration of 25–30 µg/mL in the media, while the addition of quantitative hypromellose acetate succinate (HPMCAS) MG and povidone (PVP) K30 did not alter its phase separation concentration. The second scattering dispersion phase of the system exhibited superior stability and reversibility as the formative filamentous crystalline condensates could disintegrate upon dilution. These disparate analyses consistently detected the phase separation of Axi. This manuscript could provide a better understanding of the supersaturation state of hydrophobic APIs upon pharmaceutical application. Full article
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13 pages, 1958 KiB  
Article
Assessing α-Bisabolol as a Transmucosal Permeation Enhancer of Buccal Local Anesthetics
by Renê Oliveira do Couto, Douglas Vieira Thomaz, Maira Perez Ferreira Duarte, Renata Fonseca Vianna Lopez, Vinícius Pedrazzi, Osvaldo de Freitas and Gianluca Martino Tartaglia
Pharmaceutics 2024, 16(9), 1198; https://doi.org/10.3390/pharmaceutics16091198 - 12 Sep 2024
Viewed by 1727
Abstract
Needle-free buccal anesthesia improves dental treatment outcomes for both patients and dentists. In this study, we report on an assessment of the enhancement effects of α-bisabolol on the in vitro transmucosal permeation of prilocaine hydrochloride (PCl) and lidocaine hydrochloride (LCl) from needleless buccal [...] Read more.
Needle-free buccal anesthesia improves dental treatment outcomes for both patients and dentists. In this study, we report on an assessment of the enhancement effects of α-bisabolol on the in vitro transmucosal permeation of prilocaine hydrochloride (PCl) and lidocaine hydrochloride (LCl) from needleless buccal films. We also evaluated the mechanical properties of the film, which consisted of Methocel™ K100 LV as the film-forming polymer (3% m·m−1), PEG 400 as a cosolvent (15% m·m−1 based on drug loading), α-bisabolol (15 and 30% m·m−1 based on drug loading), and the drugs combined at a 1:1 ratio (15 mg·unit−1). The porcine esophageal epithelium was used as a membrane barrier, and artificial saliva was the release medium. After a 1 h experiment at 25 ± 2 °C, α-bisabolol significantly decreased, rather than enhanced, the permeation fluxes (five-fold), permeability coefficients (seven-fold), and retentions (two-fold) of both PCl and LCl through the epithelium, regardless of the concentration. Moreover, the resistance and flexibility of the films markedly decreased compared to those without α-bisabolol. Therefore, under the experimental conditions, using α-bisabolol as a buccal permeation enhancer for the hydrophilic local anesthetics PCl and LCl from buccal films is not feasible. Full article
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14 pages, 1957 KiB  
Article
Surface Migration of Fatty Acid to Improve Sliding Properties of Hypromellose-Based Coatings
by Maurice Brogly, Sophie Bistac and Armand Fahs
Surfaces 2024, 7(3), 666-679; https://doi.org/10.3390/surfaces7030043 - 2 Sep 2024
Cited by 1 | Viewed by 1516
Abstract
Hypromellose (HM) is a cellulose-derived polymer of pharmaceutical grade that forms easily from thin films and coatings. As few studies concern HM-formulated systems, this study focuses on the formulation of HM films by incorporating a fatty acid additive, making it possible to control [...] Read more.
Hypromellose (HM) is a cellulose-derived polymer of pharmaceutical grade that forms easily from thin films and coatings. As few studies concern HM-formulated systems, this study focuses on the formulation of HM films by incorporating a fatty acid additive, making it possible to control surface properties such as wetting and slip behavior for pharmaceutical or medical applications. The results show that the addition of a very small amount (from 0.1 to 1% w/w) of fatty acid additive reduces HM film affinity for water and water vapor transmission rate, while film appearance and gloss are rather preserved. Surface properties were probed using wettability measurements, Tapping Mode AFM, ATR-FTIR spectrometry, and friction measurements. Tapping Mode AFM images show that the surface roughness reduces by up to 65%. Wettability results show that the surface energy decreases from 43 to 31 mJ.m−2, whereas surface FTIR spectrometry measurements demonstrate that fatty acid molecules migrate on the surface of the formulated films, the driving force being the microphase separation between the polar HM macromolecules and the hydrophobic additive, leading to the formation of a weak boundary layer with poor cohesion. As a consequence, the surface coefficient of friction significantly reduces from 0.38 to 0.08, and fatty acid molecules thus act as a lubricant, improving the sliding properties of HM-based coatings. Full article
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25 pages, 17518 KiB  
Article
Solid Dispersions Obtained by Ball Milling as Delivery Platform of Etodolac, a Model Poorly Soluble Drug
by Anna Czajkowska-Kośnik, Iwona Misztalewska-Turkowicz, Agnieszka Zofia Wilczewska, Anna Basa and Katarzyna Winnicka
Materials 2024, 17(16), 3923; https://doi.org/10.3390/ma17163923 - 7 Aug 2024
Cited by 2 | Viewed by 2055
Abstract
Poor water solubility of drugs is a limiting factor for their bioavailability and pharmacological activity. Many approaches are known to improve drug solubility, and among them, the physical method, solid dispersions (SDs), is applied. SDs are physical mixtures of a drug and a [...] Read more.
Poor water solubility of drugs is a limiting factor for their bioavailability and pharmacological activity. Many approaches are known to improve drug solubility, and among them, the physical method, solid dispersions (SDs), is applied. SDs are physical mixtures of a drug and a carrier, sometimes with the addition of a surfactant, which can be obtained by milling, cryomilling, spray-drying, or lyophilization processes. In this study, solid dispersions with etodolac (ETD-SDs) were prepared by the milling method using different carriers, such as hypromellose, polyvinylpyrrolidone, copovidone, urea, and mannitol. Solubility studies, dissolution tests, morphological assessment, thermal analysis, and FTIR imaging were applied to evaluate the SD properties. It was shown that the ball-milling process can be applied to obtain SDs with ETD. All designed ETD-SDs were characterized by higher water solubility and a faster dissolution rate compared to unprocessed ETD. SDs with amorphous carriers (HPMC, PVP, and PVP/VA) provided greater ETD solubility than dispersions with crystalline features (urea and mannitol). FTIR spectra confirmed the compatibility of ETD with tested carriers. Full article
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21 pages, 2588 KiB  
Article
Utilization of the Drug–Polymer Solid Dispersion Obtained by Ball Milling as a Taste Masking Method in the Development of Orodispersible Minitablets with Hydrocortisone in Pediatric Doses
by Monika Trofimiuk, Katarzyna Olechno, Emil Trofimiuk, Anna Czajkowska-Kośnik, Patrycja Ciosek-Skibińska, Klaudia Głowacz, Joanna Lenik, Anna Basa, Halina Car and Katarzyna Winnicka
Pharmaceutics 2024, 16(8), 1041; https://doi.org/10.3390/pharmaceutics16081041 - 4 Aug 2024
Cited by 2 | Viewed by 2932
Abstract
The objective of the conducted research was to design 2 mm orodispersible minitablets of pediatric doses of hydrocortisone (0.5 mg; 1.0 mg) with desirable pharmaceutical properties and eliminate the sensation of a bitter taste using preparation of solid dispersion by ball mill. Hydrocortisone [...] Read more.
The objective of the conducted research was to design 2 mm orodispersible minitablets of pediatric doses of hydrocortisone (0.5 mg; 1.0 mg) with desirable pharmaceutical properties and eliminate the sensation of a bitter taste using preparation of solid dispersion by ball mill. Hydrocortisone was selected as the model substance, as it is widely utilized in the pediatric population. ODMTs were prepared by compression (preceded by granulation) in a traditional single-punch tablet machine and evaluated using pharmacopoeial tests, DSC, and FTIR analysis. The methods used to evaluate the effectiveness of the taste-masking effect included in vivo participation of healthy volunteers, in vitro drug dissolution and utilization of an analytical device—“electronic tongue”. The research employed a preclinical animal model to preliminary investigate the bioequivalence of the designed drug dosage form in comparison to reference products. The study confirmed the possibility of manufacturing good-quality hydrocortisone ODMTs with a taste-masking effect owing to the incorporation of a solid dispersion in the tablet mass. Full article
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18 pages, 4244 KiB  
Article
Enhanced Stability and Compatibility of Montelukast and Levocetirizine in a Fixed-Dose Combination Monolayer Tablet
by Tae Han Yun, Moon Jung Kim, Jung Gyun Lee, Kyu Ho Bang and Kyeong Soo Kim
Pharmaceutics 2024, 16(7), 963; https://doi.org/10.3390/pharmaceutics16070963 - 21 Jul 2024
Cited by 3 | Viewed by 4728
Abstract
The purpose of this study was to enhance the stability of montelukast and levocetirizine for the development of a fixed-dose combination (FDC) monolayer tablet. To evaluate the compatibility of montelukast and levocetirizine, a mixture of the two drugs was prepared, and changes in [...] Read more.
The purpose of this study was to enhance the stability of montelukast and levocetirizine for the development of a fixed-dose combination (FDC) monolayer tablet. To evaluate the compatibility of montelukast and levocetirizine, a mixture of the two drugs was prepared, and changes in the appearance characteristics and impurity content were observed in a dry oven at 60 °C. Excipients that contributed minimally to impurity increases were selected to minimize drug interactions. Mannitol, microcrystalline cellulose, croscarmellose sodium, hypromellose, and sodium citrate were chosen as excipients, and montelukast–levocetirizine FDC monolayer tablets were prepared by wet granulating the two drugs separately. A separate granulation of montelukast and levocetirizine, along with the addition of sodium citrate as a pH stabilizer, minimized the changes in tablet appearance and impurity levels. The prepared tablets demonstrated release profiles equivalent to those of commercial products in comparative dissolution tests. Subsequent stability testing at 40 ± 2 °C and 75 ± 5% RH for 6 months confirmed that the drug content, dissolution rate, and impurity content met the specified acceptance criteria. In conclusion, the montelukast–levocetirizine FDC monolayer tablet developed in this study offers a potential alternative to commercial products. Full article
(This article belongs to the Special Issue Pharmaceutical Solid Forms: From Crystal Structure to Formulation)
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