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Pharmaceutics
Special Issues
Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges
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Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Clinical Pharmaceutics".

Deadline for manuscript submissions: closed (20 October 2023) | Viewed by 8355

Special Issue Editor

Dr. Anroop Nair

E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia
Interests: drug delivery; nanoformulations; drug targeting; film-based formulations; pharmacokinetics

Special Issue Information

Dear Colleagues,

Developing a new chemical entity into a pharmaceutically acceptable formulation involves numerous critically validated procedures across both preclinical and clinical investigations. As a part of the drug discovery and development program, preclinical formulations and various drug delivery approaches are being actively developed to improve the physicochemical properties and in vivo exposure of drugs to advance their pharmacodynamic and pharmacokinetic properties. Rapid advancement is anticipated in areas such as digital technology, genetics, and novel materials, and the implementation of novel technologies such as 3D printing will be of major importance in the development of stable, biopharmaceutically suitable preclinical formulations. The application of Design of Experiments (DoE), Process Analytical Technology (PAT) and Artificial Neural Networks (ANNs) has been utilized in exploring the critical process parameters that can significantly influence the quality and performance characteristics of pharmaceutical drug products.

This Special Issue aims to highlight recent research or reviews with an emphasis on the recent developments in various preclinical drug formulations or delivery systems. The authors are welcome to contribute articles related to preformulation studies or drug delivery systems, irrespective of the route of administration.

Dr. Anroop Nair
Guest Editor

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

  • drug delivery systems
  • drug targeting
  • 3D printing
  • formulation development
  • nanotechnology
  • nanocarriers
  • hydrogels
  • film
  • self-assembled nanomicelles
  • drug solubility
  • drug release kinetics
  • dissolution
  • bioavailability
  • drug stability

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Published Papers (5 papers)

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Research

16 pages, 4464 KiB  
Article
Radiofrequency Combined with Intratumoral Immunotherapy: Preclinical Results and Safety in Metastatic Colorectal Carcinoma
by Johanne Seguin, Mostafa El Hajjam, Josette Legagneux, Sarah Diakhaby, Nathalie Mignet, Vincent Boudy, Balthazar Toussaint, Frederique Peschaud, Jean François Emile, Claude Capron and Robert Malafosse
Pharmaceutics 2024, 16(3), 315; https://doi.org/10.3390/pharmaceutics16030315 - 23 Feb 2024
Viewed by 1610
Abstract
Radiofrequency ablation (RFA) of cancer induces an anti-tumor immunity, which is insufficient to prevent recurrences. In mice, RFA–intratumoral immunotherapy by granulocyte–macrophage colony-stimulating factor (GM-CSF) and Bacillus Calmette-Guerin resulted in complete metastases regression. Infectious risk in human needs replacement of live vaccines. Intratumoral purified [...] Read more.
Radiofrequency ablation (RFA) of cancer induces an anti-tumor immunity, which is insufficient to prevent recurrences. In mice, RFA–intratumoral immunotherapy by granulocyte–macrophage colony-stimulating factor (GM-CSF) and Bacillus Calmette-Guerin resulted in complete metastases regression. Infectious risk in human needs replacement of live vaccines. Intratumoral purified protein derivatives (PPD) have never been tested in digestive cancers, and the safety of intratumoral immunotherapy after RFA has not yet been validated in human models. We investigated the therapeutic efficacy of combined radiofrequency ablation (RFA) and intratumoral immunotherapy (ITI) using an immune-muco-adherent thermogel (IMT) in a mouse model of metastatic colorectal cancer (CRC) and the safety of this approach in a pig model. Intratumoral stability of the immunogel was assessed using magnetic resonance imaging (MRI) and bioluminescent imaging. Seventy-four CT26 tumor-bearing female BALB/c mice were treated with RFA either alone or in combination with intratumoral IMT. Regression of distant metastasis and survival were monitored for 60 days. Six pigs that received liver radiofrequency and intralesional IMT injections were followed for 15 days. Experimental gel embolisms were treated using an intravascular approach. Pertinent rheology of IMT was confirmed in tumors, by the signal stability during 3 days in MRI and 7 days in bioluminescence imaging. In mice, the abscopal effect of RFA–intratumoral immunotherapy resulted in regression of distant lesions completed at day 16 vs. a volume of 350 ± 99.3 mm3 in the RFA group at day 25 and a 10-fold survival rate at 60 days. In pigs, injection of immunogel in the liver RFA area was safe after volume adjustment without clinical, hematological, and liver biology disorder. Flow cytometry showed an early increase in CD3 TCRγδ+T cells at D7 (p < 0.05) and a late decrease in CD29+-CD8 T cells at D15 (p < 0.05), reflecting the inflammation status changes. Systemic GM-CSF release was not detectable. Experimental caval and pulmonary thermogel embolisms were treated by percutaneous catheterism and cold serum infusion. RFA–intratumoral immunotherapy as efficient and safe mini-invasive interventional oncology is able to improve ablative treatment of colorectal liver metastases. Full article
(This article belongs to the Special Issue Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges)
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20 pages, 5787 KiB  
Article
Cocrystallization of Gefitinib Potentiate Single-Dose Oral Administration for Lung Tumor Eradication via Unbalancing the DNA Damage/Repair
by Muhammad Inam, Yi Yang, Jialin Hu, Jiena Zheng, Wenxia Deng, You Zhou, Jialong Qi, Chuanshan Xu, Guihong Chai, Yuanye Dang and Wenjie Chen
Pharmaceutics 2023, 15(12), 2713; https://doi.org/10.3390/pharmaceutics15122713 - 30 Nov 2023
Viewed by 1321
Abstract
Gefitinib (GEF) is a clinical medication for the treatment of lung cancer targeting the epidermal growth factor receptor (EGFR). However, its efficacy is remarkably limited by low solubility and dissolution rates. In this study, two cocrystals of GEF with co-formers were successfully synthesized [...] Read more.
Gefitinib (GEF) is a clinical medication for the treatment of lung cancer targeting the epidermal growth factor receptor (EGFR). However, its efficacy is remarkably limited by low solubility and dissolution rates. In this study, two cocrystals of GEF with co-formers were successfully synthesized using the recrystallization method characterized via Powder X-ray Diffraction, Fourier Transform Infrared Spectroscopy, and 2D Nuclear Overhauser Effect Spectroscopy. The solubility and dissolution rates of cocrystals were found to be two times higher than those of free GEF. In vitro cytotoxicity studies revealed that the cocrystals enhanced the inhibition of cell proliferation and apoptosis in A549 and H1299 cells compared to free GEF. In mouse models, GEF@TSBO demonstrated targeted, safe, and effective antitumor activity with only one-dose administration. Mechanistically, the GEF cocrystals were shown to increase the cellular levels of damaged DNA, while potentially downregulating PARP, thereby impairing the DNA repair machinery and leading to an imbalance between DNA damage and restoration. These findings suggest that the cocrystallization of GEF could serve as a promising adjunct to significantly enhance the physicochemical and biopharmaceutical performance for lung cancer treatment, providing a facial strategy to improve GEF anticancer efficiency with high bioavailability that can be orally administrated with only one dose. Full article
(This article belongs to the Special Issue Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges)
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14 pages, 2953 KiB  
Article
Bovine Serum Albumin Nanoparticles Enhanced the Intranasal Bioavailability of Silybin in Rats
by Ana Paula Santos Tartari, Samila Horst Peczek, Margani Taise Fin, Jeferson Ziebarth, Christiane Schineider Machado and Rubiana Mara Mainardes
Pharmaceutics 2023, 15(12), 2648; https://doi.org/10.3390/pharmaceutics15122648 - 21 Nov 2023
Cited by 1 | Viewed by 1184
Abstract
Silybin (SLB), an important flavonoid from silymarin, displays significant hepatoprotective, anticancer, antioxidant, and neuroprotective effects. However, its therapeutic efficacy is limited by its low solubility and bioavailability. To address these challenges, we engineered bovine serum albumin (BSA) nanoparticles (NP) loaded with SLB (BSA-NP/SLB) [...] Read more.
Silybin (SLB), an important flavonoid from silymarin, displays significant hepatoprotective, anticancer, antioxidant, and neuroprotective effects. However, its therapeutic efficacy is limited by its low solubility and bioavailability. To address these challenges, we engineered bovine serum albumin (BSA) nanoparticles (NP) loaded with SLB (BSA-NP/SLB) using the coacervation method. BSA-SLB NP exhibited a spherical shape, a mean size of 197 nm, a polydispersity index of 0.275, a zeta potential of −34 mV, and an entrapment efficiency of 67%. X-ray diffraction analysis indicated amorphization of SLB upon encapsulation. Formulation stability was upheld over 180 days. In vitro release assays demonstrated controlled diffusion-erosion release, with approximately 40% SLB released within 0.5 h and 100% over 12 h. Intranasal administration of BSA-NP/SLB in rats improved SLB bioavailability by fourfold compared to free SLB. These findings highlight the promising potential of intranasally administered BSA-NP/SLB as an alternative approach to enhance SLB bioavailability, paving the way for innovative therapeutic applications. Full article
(This article belongs to the Special Issue Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges)
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26 pages, 6089 KiB  
Article
Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers
by Fahad Mohammed AlMulhim, Anroop B. Nair, Bandar Aldhubiab, Hiral Shah, Jigar Shah, Vivek Mewada, Nagaraja Sreeharsha and Shery Jacob
Pharmaceutics 2023, 15(11), 2530; https://doi.org/10.3390/pharmaceutics15112530 - 25 Oct 2023
Cited by 2 | Viewed by 1634
Abstract
The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured lipid carriers (NLCs) and [...] Read more.
The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured lipid carriers (NLCs) and assesses the potential to enhance its bioavailability. Box–Behnken-based design optimization of NLCs was performed by examining the particles’ physical characteristics. The polymeric film was used to load optimized NLCs, which were then assessed for their pharmaceutical properties, permeability, and pharmacokinetics. The optimization outcomes indicated that selected formulation variables had a considerable (p < 0.05) impact on responses such as particle size, entrapment efficiency, and % drug release. Desired characteristics such as a negative charge, higher entrapment efficiency, and nanoparticles with ideal size distribution were shown by optimized NLC dispersions. The developed film demonstrated excellent physico-mechanical properties, appropriate texture, good drug excipient compatibility (chemically stable formulation), and amorphous drug nature. A sustained Weibull model drug release (p < 0.0005) and superior flux (~5-fold higher, p < 0.005) were seen in NLC-loaded film compared to plain-drug-loaded film. The pharmacokinetics profile in rabbits supports the goal of buccal therapy as evidenced by significantly higher AUC0–12 (p < 0.0001) and greater relative bioavailability (236%) than the control. These results support the conclusion that paliperidone-loaded NLC buccal film has the potential to be an alternate therapy for its effective administration in the treatment of schizophrenia. Full article
(This article belongs to the Special Issue Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges)
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13 pages, 2412 KiB  
Article
Injectable pH and Thermo-Responsive Hydrogel Scaffold with Enhanced Osteogenic Differentiation of Preosteoblasts for Bone Regeneration
by Jasmine L. King, Roopali Shrivastava, Pooja D. Shah, Panita Maturavongsadit and Soumya Rahima Benhabbour
Pharmaceutics 2023, 15(9), 2270; https://doi.org/10.3390/pharmaceutics15092270 - 2 Sep 2023
Viewed by 1466
Abstract
Bone fractures are common in the geriatric population and pose a great economic burden worldwide. While traditional methods for repairing bone defects have primarily been autografts, there are several drawbacks limiting its use. Bone graft substitutes have been used as alternative strategies to [...] Read more.
Bone fractures are common in the geriatric population and pose a great economic burden worldwide. While traditional methods for repairing bone defects have primarily been autografts, there are several drawbacks limiting its use. Bone graft substitutes have been used as alternative strategies to improve bone healing. However, there remain several impediments to achieving the desired healing outcomes. Injectable hydrogels have become attractive scaffold materials for bone regeneration, given their high performance in filling irregularly sized bone defects and their ability to encapsulate cells and bioactive molecules and mimic the native ECM of bone. We investigated the use of an injectable chitosan-based hydrogel scaffold to promote the differentiation of preosteoblasts in vitro. The hydrogels were characterized by evaluating cell homogeneity, cell viability, rheological and mechanical properties, and differentiation ability of preosteoblasts in hydrogel scaffolds. Cell-laden hydrogel scaffolds exhibited shear thinning behavior and the ability to maintain shape fidelity after injection. The CNC-CS hydrogels exhibited higher mechanical strength and significantly upregulated the osteogenic activity and differentiation of preosteoblasts, as shown by ALP activity assays and histological analysis of hydrogel scaffolds. These results suggest that this injectable hydrogel is suitable for cell survival, can promote osteogenic differentiation of preosteoblasts, and structurally support new bone growth. Full article
(This article belongs to the Special Issue Novel Preclinical Drug Formulation and Delivery Approaches: Developments and Challenges)
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