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Pharmaceutics
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Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of...
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Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine

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

Deadline for manuscript submissions: 30 September 2024 | Viewed by 3769

Special Issue Editors

Dr. Hamdy Abdelkader

E-Mail Website
Guest Editor
Pharmaceutics Department, College of Pharmacy, King Khalid University, Abha 62223, Saudi Arabia
Interests: preformulation studies; cyclodextrins; solubility enhancement; modified release systems; niosomes; ocular delivery; irritation models
Special Issues, Collections and Topics in MDPI journals
Dr. Adel Al-Fatease

E-Mail Website
Guest Editor
Pharmaceutics Department, College of Pharmacy, King Khalid University, Abha 62223, Saudi Arabia
Interests: drug delivery; cancer; pancreatic diseases; bioprinting; biosensor; nanotechnology
Special Issues, Collections and Topics in MDPI journals
Dr. Zimei Wu

E-Mail Website
Guest Editor
School of Pharmacy, Faculty of Medical and Health Sciences, The University of Auckland, Auckland 1142, New Zealand
Interests: cancer nanomedicine; cytoplasmic drug delivery; targeted drug delivery; blood-brain barrier; ligand functionalised nanoparticles; liposomes; exosomes; extracellular vesicles

Special Issue Information

Dear Colleagues,

Conventional pharmaceutical excipients have been used to alter palatability, processing ability, flowability, and compressibility of dosage forms during manufacturing stages for producing elegant pharmaceutical products. Typical examples of these excipients include diluent, disintegrant, binder, lubricant, and glidant. Other pharmaceutical ingredients/excipients have been included to improve the chemical, physical, and microbial stability of the dosage forms.  The literature has reported many drug–excipient incompatibilities and excipients-related side effects such as local irritation, interference at the absorption sites through affecting efflux pumps and g-glycoproteins, and other systemic toxicities.

With the recent advances in pharmaceutical and medical sciences, active pharmaceutical agents have been launched into the market with inherent poor biopharmaceutics properties such as low solubility and limited permeability. Erratic drug absorption, inconsistent bioavailability, irritation, and poor pharmacokinetics may occur, leading to suboptimal efficacy and adverse drug reactions.

Biofunctional excipients have recently emerged, such as smart polymers, lipids, and other safe and natural additives that can alter drug solubility, release characteristics, permeability, and pharmacokinetic profiles. Typical example include in situ forming polymers, amino acids, cyclodextrins, and many more.

The new knowledge obtained from novel research ideas and manuscripts will contribute to improving bioavailability, reducing adverse effects, achieving drug targeting, or promoting better patient treatment adherence.

The focus of this Special Issue is on recent developments in biofunctional non-active ingredients/excipients used to design pharmaceutical formulations and delivery systems (for topical or systemic routes) that could confer targeted drug delivery or modified drug release to enhance efficacy, reduce irritation at the absorption site, and beyond.

We would be much appreciating if you would consider being one of our authors contributing to this Special Issue.  All types of submissions are welcome, including original research articles and comprehensive reviews.

Dr. Hamdy Abdelkader
Dr. Adel Al-Fatease
Dr. Zimei Wu
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

  • excipients
  • in situ forming polymers
  • modified-release
  • cyclodextrins
  • amino acids
  • eye diseases
  • diabetes
  • cancer

Published Papers (4 papers)

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Research

18 pages, 4654 KiB  
Article
Polymeric Amorphous Solid Dispersions of Dasatinib: Formulation and Ecotoxicological Assessment
by Katarina Sokač, Martina Miloloža, Dajana Kučić Grgić and Krunoslav Žižek
Pharmaceutics 2024, 16(4), 551; https://doi.org/10.3390/pharmaceutics16040551 - 18 Apr 2024
Viewed by 688
Abstract
Dasatinib (DAS), a potent anticancer drug, has been subjected to formulation enhancements due to challenges such as significant first-pass metabolism, poor absorption, and limited oral bioavailability. To improve its release profile, DAS was embedded in a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP). [...] Read more.
Dasatinib (DAS), a potent anticancer drug, has been subjected to formulation enhancements due to challenges such as significant first-pass metabolism, poor absorption, and limited oral bioavailability. To improve its release profile, DAS was embedded in a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP). Drug amorphization was induced in a planetary ball mill by solvent-free co-grinding, facilitating mechanochemical activation. This process resulted in the formation of amorphous solid dispersions (ASDs). The ASD capsules exhibited a notable enhancement in the release rate of DAS compared to capsules containing the initial drug. Given that anticancer drugs often undergo limited metabolism in the body with unchanged excretion, the ecotoxicological effect of the native form of DAS was investigated as well, considering its potential accumulation in the environment. The highest ecotoxicological effect was observed on the bacteria Vibrio fischeri, while other test organisms (bacteria Pseudomonas putida, microalgae Chlorella sp., and duckweed Lemna minor) exhibited negligible effects. The enhanced drug release not only contributes to improved oral absorption but also has the potential to reduce the proportion of DAS that enters the environment through human excretion. This comprehensive approach highlights the significance of integrating advances in drug development while considering its environmental implications. Full article
(This article belongs to the Special Issue Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine)
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20 pages, 1877 KiB  
Article
Conjugated Linoleic Acid–Carboxymethyl Chitosan Polymeric Micelles to Improve the Solubility and Oral Bioavailability of Paclitaxel
by Iqra Mubeen, Ghulam Abbas, Shahid Shah and Abdullah A Assiri
Pharmaceutics 2024, 16(3), 342; https://doi.org/10.3390/pharmaceutics16030342 - 28 Feb 2024
Viewed by 692
Abstract
Oral delivery, the most common method of therapeutic administration, has two significant obstacles: drug solubility and permeability. The challenges of current oral medicine delivery are being tackled through an emerging method that uses structures called polymeric micelles. In the present study, polymeric micelles [...] Read more.
Oral delivery, the most common method of therapeutic administration, has two significant obstacles: drug solubility and permeability. The challenges of current oral medicine delivery are being tackled through an emerging method that uses structures called polymeric micelles. In the present study, polymeric micelles were developed using conjugates of linoleic acid–carboxymethyl chitosan (LA-CMCS) for the oral delivery of paclitaxel (PCL). The developed micelles were evaluated by particle size, zeta potential, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). When PCL was contained within micelles, its solubility increased by almost 13.65 times (around 60 µg/mL). The micelles’ zeta potentials were −29 mV, their polydispersity indices were 0.023, and their particle diameters were 93 nm. Micelles showed PCL loading and entrapment efficiencies of 67% and 61%, respectively. The sustained release qualities of the PCL release data from micelles were good. In comparison to the pure PCL suspension, the permeability of the PCL from micelles was 2.2 times higher. The pharmacokinetic data revealed that PCL with LA-CMCS micelles had a relative bioavailability of 239.17%, which was much greater than the PCL in the suspension. The oral bioavailability of PCL was effectively increased by LA-CMCS micelles according to an in vivo study on animals. The polymer choice, maybe through improved permeability, plays an essential role when assessing oral bioavailability enhancement and solubility improvement (13.65 times). The outcomes demonstrated that PCL’s solubility and pharmacokinetics were improved in the micelles of the LA-CMCS conjugate. Full article
(This article belongs to the Special Issue Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine)
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20 pages, 8957 KiB  
Article
Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance
by Barzan Osi, Ali A. Al-Kinani, Zinah K. Al-Qaysi, Mouhamad Khoder and Raid G. Alany
Pharmaceutics 2024, 16(1), 112; https://doi.org/10.3390/pharmaceutics16010112 - 15 Jan 2024
Viewed by 847
Abstract
Rho-kinase (ROCK) inhibitors represent a new category of anti-glaucoma medications. Among them, Fasudil hydrochloride, a selective ROCK inhibitor, has demonstrated promising outcomes in glaucoma treatment. It works by inhibiting the ROCK pathway, which plays a crucial role in regulating the trabecular meshwork and [...] Read more.
Rho-kinase (ROCK) inhibitors represent a new category of anti-glaucoma medications. Among them, Fasudil hydrochloride, a selective ROCK inhibitor, has demonstrated promising outcomes in glaucoma treatment. It works by inhibiting the ROCK pathway, which plays a crucial role in regulating the trabecular meshwork and canal of Schlemm’s aqueous humor outflow. This study aims to investigate the ocular absorption pathway of Fasudil hydrochloride and, subsequently, develop a nanoparticle-based delivery system for enhanced corneal absorption. Employing the ionic gelation method and statistical experimental design, the factors influencing chitosan nanoparticle (Cs NP) characteristics and performance were explored. Fasudil in vitro release and ex vivo permeation studies were performed, and Cs NP ocular tolerability and cytotoxicity on human lens epithelial cells were evaluated. Permeation studies on excised bovine eyes revealed significantly higher Fasudil permeation through the sclera compared to the cornea (370.0 μg/cm2 vs. 96.8 μg/cm2, respectively). The nanoparticle size (144.0 ± 15.6 nm to 835.9 ± 23.4 nm) and entrapment efficiency range achieved (17.2% to 41.4%) were predominantly influenced by chitosan quantity. Cs NPs showed a substantial improvement in the permeation of Fasudil via the cornea, along with slower release compared to the Fasudil aqueous solution. The results from the Hen’s Egg Test Chorioallantoic Membrane (HET-CAM) and Bovine Corneal Opacity and Permeability (BCOP) tests indicated good conjunctival and corneal biocompatibility of the formulated chitosan nanoparticles, respectively. Lens epithelial cells displayed excellent tolerance to low concentrations of these nanoparticles (>94% cell viability). To the best of our knowledge, this is the first report on the ocular absorption pathway of topically applied Fasudil hydrochloride where the cornea has been identified as a potential barrier that could be overcome using Cs NPs. Full article
(This article belongs to the Special Issue Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine)
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19 pages, 4607 KiB  
Article
Effect of Phenolics from Aeonium arboreum on Alpha Glucosidase, Pancreatic Lipase, and Oxidative Stress; a Bio-Guided Approach
by Marwah M. Alfeqy, Seham S. El-Hawary, Ali M. El-Halawany, Mohamed A. Rabeh, Saad A. Alshehri, Aya M. Serry, Heba A. Fahmy and Marwa. I. Ezzat
Pharmaceutics 2023, 15(11), 2541; https://doi.org/10.3390/pharmaceutics15112541 - 27 Oct 2023
Viewed by 865
Abstract
Metabolic syndrome (MetS) is a global issue affecting over a billion people, raising the risk of diabetes, cardiovascular disorders, and other ailments. It is often characterized by hypertension, dyslipidemia and/or obesity, and hyperglycemia. Chemical investigation of Aeonium arboreum (L.) Webb & Berthel led [...] Read more.
Metabolic syndrome (MetS) is a global issue affecting over a billion people, raising the risk of diabetes, cardiovascular disorders, and other ailments. It is often characterized by hypertension, dyslipidemia and/or obesity, and hyperglycemia. Chemical investigation of Aeonium arboreum (L.) Webb & Berthel led to the isolation of six compounds, viz. β-sitosterol, β-sitosterol glucoside, myricetin galactoside, quercetin rhamnoside, kaempferol rhamnoside, and myricetin glucoside. Interestingly, A. arboreum’s dichloromethane (DCM), 100 and 50% MeOH Diaion fractions and the isolated compound (quercetin-3-rhamnoside) revealed potent α-glucosidase inhibitory activity, especially 50% Diaion fraction. In addition, they also showed very potent antioxidant potential, especially the polar fractions, using DPPH, ABTS, FRAP, ORAC, and metal chelation assays. Notably, the 50% Diaion fraction had the highest antioxidant potential using DPPH and ORAC assays, while the 100% Diaion fraction and quercetin-3-rhamnoside showed the highest activity using ABTS, FRAP, and metal chelation assays. Also, quercetin-3-rhamnoside showed a good docking score of −5.82 kcal/mol in comparison to acarbose. In addition, molecular dynamic stimulation studies illustrated high stability of compound binding to pocket of protein. Such potent activities present A. arboreum as a complementary safe approach for the management of diabetes mellitus as well as MetS. Full article
(This article belongs to the Special Issue Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine)
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