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Pharmaceutics
Special Issues
Improving the Bioavailability and Solubility of Pharmaceutical Formulations
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Improving the Bioavailability and Solubility of Pharmaceutical Formulations

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: 10 March 2026 | Viewed by 7233

Special Issue Editors

Dr. Zoltan Ujhelyi

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Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, 4032 Debrecen, Hungary
Interests: pharmaceutical research and development; nanotechnology; permeability enhancement
Special Issues, Collections and Topics in MDPI journals
Dr. Dóra Kósa

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Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary
Interests: bioavailability enhancement; oral formulations; micro- and nanotechnology; peptide carriers; biocompatibility
Dr. Ágota Pető

E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary
Interests: bioavailability enhancement; topical formulations; nanotechnology; transdermal patches; in vitro permeation

Special Issue Information

Dear Colleagues,

In modern pharmacotherapy, there is an increasing demand to develop new pharmaceutical forms that can be safely administered with adequate bioavailability and patient compliance in order to achieve successful therapeutic responses. Bioavailability is essential in the development of new drugs and formulations. More effective and efficient active ingredients can be designed by understanding the factors that affect bioavailability, such as solubility, chemical stability, and pharmaceutical forms. This leads to innovative drugs with higher bioavailability and a better therapeutic profile. In order to reach the site of action and achieve the required pharmacological effect, drugs have to face biological membranes, regardless of the route of administration. Overall, many methods and innovative dosage forms have been developed in the last decade to overcome these challenges.

This Special Issue aims to highlight the key aspects of recent techniques and methods used to improve the bioavailability of active pharmaceutical ingredients, as well as enhance the solubility and dissolution of poorly soluble pharmacons. In this Special Issue, we welcome researchers to contribute original research and review articles relevant to this topic.

We look forward to receiving your contributions.

Dr. Zoltan Ujhelyi
Dr. Dóra Kósa
Dr. Ágota Pető
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • bioavailability enhancement
  • drug delivery systems
  • in vitro and in vivo evaluation methods
  • therapeutic effectiveness
  • pharmaceutical innovations
  • nanoformulations
  • surfactants
  • poorly soluble drugs

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Published Papers (5 papers)

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Research

20 pages, 2208 KiB  
Article
Food Effect and Formulation: How Soluble Fillers Affect the Disintegration and Dissolution of Tablets in Viscous Simulated Fed State Media
by Muhammad Farooq Umer, Valentin Stahl, Jozef Al-Gousous, Thomas Nawroth, Wei-Jhe Sun, Fang Wu, Wenlei Jiang, Zongming Gao and Peter Langguth
Pharmaceutics 2025, 17(5), 567; https://doi.org/10.3390/pharmaceutics17050567 - 25 Apr 2025
Viewed by 346
Abstract
The food-induced viscosity of the media can alter tablet disintegration and eventually the release of the drug it contains. The extent of this retardation depends on tablet formulation factors, such as the solubility of its excipients. Objectives: This research aimed to study [...] Read more.
The food-induced viscosity of the media can alter tablet disintegration and eventually the release of the drug it contains. The extent of this retardation depends on tablet formulation factors, such as the solubility of its excipients. Objectives: This research aimed to study the effect of filler solubility on the disintegration and dissolution of tablets under different testing conditions. Methods: Tablet formulations containing acetaminophen (as a model compound), mixtures of different ratios of fillers, and other excipients were directly compressed using uniform manufacturing parameters. These formulations were investigated under fasted- and fed-state conditions to determine the influence of viscosity on their disintegration, inspired by the liquid penetration ratio (LPR) theoretical framework. Disintegration and dissolution tests were performed using both compendial and novel testing apparatuses. Results: The soluble fillers in the tablets affected their disintegration and dissolution in the simulated fed-state medium, while fasted-state conditions affected the tablets only marginally. The testing devices showed partially contrasting results, which appeared to be due to the hydrodynamics of the testing media used. The novel CNC (computed numerical control) apparatus offered 3D motion and effectively exposed the tablets to the viscous testing media, unlike the compendial paddle apparatus. Conclusions: This study explored the impact of filler solubility on the disintegration and dissolution of tablets. As the LPR framework revealed, fillers with a higher solubility have positive effects on the disintegration and dissolution of tablets in viscous conditions. Additionally, the proportion of soluble filler used is also inversely correlated with the disintegration time. Further investigation of the formulation parameters, as well as the testing conditions, would provide additional insights into the effects of food on these tablets. Full article
(This article belongs to the Special Issue Improving the Bioavailability and Solubility of Pharmaceutical Formulations)
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21 pages, 4633 KiB  
Article
Alectinib-Loaded Chitosan–Alginate Nanoparticles: A Novel Synthesis Method with In Vitro and In Vivo Evaluations
by Tha’er Ata, Israa Al-Ani, Nida Karameh, Mahmood R. Atta and Wael Abu Dayyih
Pharmaceutics 2025, 17(4), 492; https://doi.org/10.3390/pharmaceutics17040492 - 8 Apr 2025
Viewed by 1645
Abstract
Background/Objectives: Non-small cell lung cancer (NSCLC) constitutes over 84% of all lung cancer cases and is a leading cause of cancer-related mortality globally. Alectinib, a second-generation anaplastic lymphoma kinase (ALK) inhibitor, is effective in ALK-positive NSCLC; however, its clinical potential is hampered [...] Read more.
Background/Objectives: Non-small cell lung cancer (NSCLC) constitutes over 84% of all lung cancer cases and is a leading cause of cancer-related mortality globally. Alectinib, a second-generation anaplastic lymphoma kinase (ALK) inhibitor, is effective in ALK-positive NSCLC; however, its clinical potential is hampered by poor aqueous solubility and limited oral bioavailability. This study aimed to develop Alectinib-loaded chitosan–alginate nanoparticles (ACANPs) to enhance its solubility, oral bioavailability, and therapeutic efficacy. Methods: ACANPs were synthesized using a novel combined solid/oil/water (s/o/w) emulsification technique with ionotropic gelation. Characterization was performed using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), dynamic light scattering (DLS), and zeta potential measurements. A validated high-performance liquid chromatography (HPLC) method quantified the Alectinib. In vitro drug release studies compared free Alectinib with ACANPs. Cytotoxicity against NSCLC cell lines (A549 and H460) was assessed using MTT assays. Pharmacokinetic parameters were evaluated in rats using LC–MS/MS. Results: ACANPs showed a high encapsulation efficiency (~97%), an average particle size of 161 nm, and a positive zeta potential of +21 mV. In vitro release studies revealed a threefold increase in drug release from ACANPs over 48 h compared to free Alectinib. Cytotoxicity assays demonstrated significantly reduced IC50 values for ACANPs. Pharmacokinetic analyses showed an enhanced maximum plasma concentration (Cmax) and area under the curve (AUC), indicating a 78% increase in oral bioavailability. Conclusions: ACANPs substantially improved the solubility, cytotoxic efficacy, and oral bioavailability of Alectinib, suggesting their potential as a promising nanocarrier system for enhancing NSCLC treatment outcomes. Full article
(This article belongs to the Special Issue Improving the Bioavailability and Solubility of Pharmaceutical Formulations)
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22 pages, 3664 KiB  
Article
Formulation and Evaluation of Polymeric Spherical Agglomerates-Based Porous Orodispersible Tablets of Cilnidipine
by Yahya Alhamhoom, Sanjana S. Prakash, Avichal Kumar, Shivakumar Hagalavadi Nanjappa, Mohamed Rahamathulla, Megha S. Kamath, Syeda Ayesha Farhana, Mohammed Muqtader Ahmed and Thippeswamy Boreddy-Shivanandappa
Pharmaceutics 2025, 17(2), 170; https://doi.org/10.3390/pharmaceutics17020170 - 28 Jan 2025
Viewed by 1381
Abstract
Background/Objectives: Cilnidipine (CIL) is a calcium channel blocker that exhibits low bioavailability (~13%) due to poor aqueous solubility and extensive pre-systemic gut wall metabolism. The current study aimed to enhance the oral bioavailability of CIL by formulation of polymeric spherical agglomerates (CILSAs)-based orodispersible [...] Read more.
Background/Objectives: Cilnidipine (CIL) is a calcium channel blocker that exhibits low bioavailability (~13%) due to poor aqueous solubility and extensive pre-systemic gut wall metabolism. The current study aimed to enhance the oral bioavailability of CIL by formulation of polymeric spherical agglomerates (CILSAs)-based orodispersible tablets (ODTs). Methods: Eight different batches of CILSAs were prepared by a crystallo-co-agglomeration technique using different proportions of hydrophilic polymers like hydroxy propyl methyl cellulose E50, polyvinyl pyrrolidone K30, or polyethylene glycol (PEG) 6000 as carriers. Fourier transform infrared spectroscopy (FTIR) of CILSAs proved the chemical integrity of CIL in SAs, while scanning electron microscopy revealed the spherical shape of CILSAs. Results: Differential scanning calorimetry and powder X-ray diffraction studies confirmed that CIL was rendered more amorphous in CILSAs. CILSAs displayed good flow behavior, high percentage yield, and high drug loads. The batch F4 composed of PEG 6000 emerged as the optimized batch as it displayed high percentage dissolution efficiency (57.01 ± 0.01%), which was significantly greater (p < 0.001) compared to CIL (26.27 ± 0.06%). The optimized formulation of CILSAs was directly compressed into ODTs that were rendered porous by vacuum drying. The optimized formulation of porous ODTs (T3) displayed low friability (0.28 ± 0.03%), short disintegration time (6.26 ± 0.29 s), and quicker dissolution (94.16 ± 1.41% in 60 min) as compared to marketed tablet Cildipin® 10 mg (85 ± 2.3%). Conclusions: Thus, porous ODTs of CILSAs can rapidly release the drug, bypass gut metabolism, enhance oral bioavailability, and improve CIL’s therapeutic effectiveness for angina and hypertension. Full article
(This article belongs to the Special Issue Improving the Bioavailability and Solubility of Pharmaceutical Formulations)
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20 pages, 3753 KiB  
Article
Twin Screw Melt Granulation of Simvastatin: Drug Solubility and Dissolution Rate Enhancement Using Polymer Blends
by Rasha M. Elkanayati, Indrajeet Karnik, Prateek Uttreja, Nagarjuna Narala, Sateesh Kumar Vemula, Krizia Karry and Michael A. Repka
Pharmaceutics 2024, 16(12), 1630; https://doi.org/10.3390/pharmaceutics16121630 - 23 Dec 2024
Cited by 1 | Viewed by 1493
Abstract
Background/Objectives: This study evaluates the efficacy of twin screw melt granulation (TSMG), and hot-melt extrusion (HME) techniques in enhancing the solubility and dissolution of simvastatin (SIM), a poorly water-soluble drug with low bioavailability. Additionally, the study explores the impact of binary polymer blends [...] Read more.
Background/Objectives: This study evaluates the efficacy of twin screw melt granulation (TSMG), and hot-melt extrusion (HME) techniques in enhancing the solubility and dissolution of simvastatin (SIM), a poorly water-soluble drug with low bioavailability. Additionally, the study explores the impact of binary polymer blends on the drug’s miscibility, solubility, and in vitro release profile. Methods: SIM was processed with various polymeric combinations at a 30% w/w drug load, and a 1:1 ratio of binary polymer blends, including Soluplus® (SOP), Kollidon® K12 (K12), Kollidon® VA64 (KVA), and Kollicoat® IR (KIR). The solid dispersions were characterized using modulated differential scanning calorimetry (M-DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FTIR). Dissolution studies compared the developed formulations against a marketed product. Results: The SIM-SOP/KIR blend showed the highest solubility (34 µg/mL), achieving an approximately 5.5-fold enhancement over the pure drug. Dissolution studies showed that SIM-SOP/KIR formulations had significantly higher release profiles than the physical mixture (PM) and pure drug (p < 0.01). Additionally, their release was similar to a marketed formulation, with 100% drug release within 30 min. In contrast, the SIM-K12/KIR formulation exhibited strong miscibility, but limited solubility and slower release rates, suggesting that high miscibility does not necessarily correlate with improved solubility. Conclusions: This study demonstrates the effectiveness of TSMG, and HME as effective continuous manufacturing technologies for improving the therapeutic efficacy of poorly water-soluble drugs. It also emphasizes the complexity of polymer–drug interactions and the necessity of carefully selecting compatible polymers to optimize the quality and performance of pharmaceutical formulations. Full article
(This article belongs to the Special Issue Improving the Bioavailability and Solubility of Pharmaceutical Formulations)
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26 pages, 2429 KiB  
Article
Controlling the Solubility, Release Rate and Permeation of Riluzole with Cyclodextrins
by Tatyana Volkova, Olga Simonova and German Perlovich
Pharmaceutics 2024, 16(6), 757; https://doi.org/10.3390/pharmaceutics16060757 - 3 Jun 2024
Cited by 4 | Viewed by 1206
Abstract
Riluzole (RLZ), a sodium channel-blocking benzothiazole anticonvulsant BCS class II drug, is very slightly soluble in aqueous medium. To improve aqueous solubility and modulate dissolution rate and membrane permeability, complex formation of RLZ with two cyclodextrin, α-cyclodextrin (α-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD), was studied. [...] Read more.
Riluzole (RLZ), a sodium channel-blocking benzothiazole anticonvulsant BCS class II drug, is very slightly soluble in aqueous medium. To improve aqueous solubility and modulate dissolution rate and membrane permeability, complex formation of RLZ with two cyclodextrin, α-cyclodextrin (α-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD), was studied. The stability constants demonstrated a greater affinity of SBE-β-CD towards RLZ compared to α-CD. A solubility growth of 1.7-fold and 3.7-fold with α-CD and SBE-β-CD, respectively, was detected in the solutions of 1% cyclodextrins and accompanied by the permeability reduction. For 1% CD solutions, several biopolymers (1% w/v) were tested for the membrane permeability under static conditions. The synergistic positive effect of α-CD and polymer on the solubility accompanied by unchanged permeability was revealed in RLZ/α-CD/PG, RLZ/α-CD/PEG400, and RLZ/α-CD/PEG1000 systems. Solid RLZ/CD complexes were prepared. Dynamic dissolution/permeation experiments for the solid samples disclosed the characteristic features of the release processes and permeation rate through different artificial membranes. The maximal permeation rate was determined across the hydrophilic semi-permeable cellulose membrane followed by the lipophilic PermeaPad barrier (model of intestinal and buccal absorption) and polydimethylsiloxane-polycarbonate membrane (simulating transdermal delivery way). Different mode of the permeation between the membranes was estimated and discussed. Full article
(This article belongs to the Special Issue Improving the Bioavailability and Solubility of Pharmaceutical Formulations)
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