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Drug Discovery and Delivery Systems

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 March 2022) | Viewed by 16877

Special Issue Editors

Department of Pharmaceutics, King Saud University, Riyadh 11451, Saudi Arabia
Interests: drug delivery; emulgel; phytopharmaceuticals
Department of Pharmaceutics, Ground Floor, Office # AA 90, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
Interests: thermodynamic solubility; solid dispersion; pharmacokinetic; nanoformulation

Special Issue Information

Dear Colleagues,

For this issue of Molecules, we are interested in high-quality publications (e.g., research, reviews) covering all aspects of nano-based delivery systems for the treatment of different diseases. There are numerous drug delivery systems focused on the designing of novel delivery systems with the main focus on their application to disease conditions. Conventional delivery systems have many challenges such as side effects, high dosing and toxicity. The entrapment of drugs in the nanodelivery systems offers numerous advantages of increased solubility, targeted delivery, imaging, lesser toxicity and enhanced therapeutic efficacy. This Special Issue also covers the research/reviews addressing the delivery systems that present other relevant contributions to the field of nanomedicines.

Dr. Syed Imam
Dr. Sultan Alshehri
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • nanoparticulate drug delivery
  • solubility enhancement
  • drug targeting
  • theranostic
  • cancer delivery
  • nanomedicine
  • pharmacokinetic
  • devices to drug delivery
  • protein delivery

Published Papers (7 papers)

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Research

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16 pages, 4006 KiB  
Article
Formulation and Optimization of Alogliptin-Loaded Polymeric Nanoparticles: In Vitro to In Vivo Assessment
by Dibyalochan Mohanty, Sadaf Jamal Gilani, Ameeduzzafar Zafar, Syed Sarim Imam, Ladi Alik Kumar, Mohammed Muqtader Ahmed, Mohammed Asadullah Jahangir, Vasudha Bakshi, Wasim Ahmad and Eyman Mohamed Eltayib
Molecules 2022, 27(14), 4470; https://doi.org/10.3390/molecules27144470 - 13 Jul 2022
Cited by 4 | Viewed by 1774
Abstract
The nano-drug delivery system has gained greater acceptability for poorly soluble drugs. Alogliptin (ALG) is a FDA-approved oral anti-hyperglycemic drug that inhibits dipeptidyl peptidase-4. The present study is designed to prepare polymeric ALG nanoparticles (NPs) for the management of diabetes. ALG-NPs were prepared [...] Read more.
The nano-drug delivery system has gained greater acceptability for poorly soluble drugs. Alogliptin (ALG) is a FDA-approved oral anti-hyperglycemic drug that inhibits dipeptidyl peptidase-4. The present study is designed to prepare polymeric ALG nanoparticles (NPs) for the management of diabetes. ALG-NPs were prepared using the nanoprecipitation method and further optimized by Box–Behnken experimental design (BBD). The formulation was optimized by varying the independent variables Eudragit RSPO (A), Tween 20 (B), and sonication time (C), and the effects on the hydrodynamic diameter (Y1) and entrapment efficiency (Y2) were evaluated. The optimized ALG-NPs were further evaluated for in vitro release, intestinal permeation, and pharmacokinetic and anti-diabetic activity. The prepared ALG-NPs show a hydrodynamic diameter of between 272.34 nm and 482.87 nm, and an entrapment efficiency of between 64.43 and 95.21%. The in vitro release data of ALG-NPs reveals a prolonged release pattern (84.52 ± 4.1%) in 24 h. The permeation study results show a 2.35-fold higher permeation flux than pure ALG. ALG-NPs exhibit a significantly (p < 0.05) higher pharmacokinetic profile than pure ALG. They also significantly (p < 0.05) reduce the blood sugar levels as compared to pure ALG. The findings of the study support the application of ALG-entrapped Eudragit RSPO nanoparticles as an alternative carrier for the improvement of therapeutic activity. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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15 pages, 1839 KiB  
Article
Formulation of Isopropyl Isothiocyanate Loaded Nano Vesicles Delivery Systems: In Vitro Characterization and In Vivo Assessment
by Chandra Kala, Mohammad Asif, Sadaf Jamal Gilani, Syed Sarim Imam, Najam Ali Khan, Mohamad Taleuzzaman, Ameeduzzafar Zafar, Mohammed Muqtader Ahmed, Sultan Alshehri and Mohammed M. Ghoneim
Molecules 2022, 27(9), 2876; https://doi.org/10.3390/molecules27092876 - 30 Apr 2022
Viewed by 1444
Abstract
Isopropyl Isothiocyanate (IPI) is a poorly water-soluble drug used in different biological activities. So, the present work was designed to prepare and evaluate IPI loaded vesicles and evaluated for vesicle size, polydispersity index (PDI) and zeta potential, encapsulation efficiency, drug release, and drug [...] Read more.
Isopropyl Isothiocyanate (IPI) is a poorly water-soluble drug used in different biological activities. So, the present work was designed to prepare and evaluate IPI loaded vesicles and evaluated for vesicle size, polydispersity index (PDI) and zeta potential, encapsulation efficiency, drug release, and drug permeation. The selected formulation was coated with chitosan and further assessed for the anti-platelet and anti-thrombotic activity. The prepared IPI vesicles (F3) exhibited a vesicle size of 298 nm ± 5.1, the zeta potential of −18.7 mV, encapsulation efficiency of 86.2 ± 5.3% and PDI of 0.33. The chitosan-coated IPI vesicles (F3C) exhibited an increased size of 379 ± 4.5 nm, a positive zeta potential of 23.5 ± 2.8 mV and encapsulation efficiency of 77.3 ± 4.1%. IPI chitosan vesicle (F3C) showed enhanced mucoadhesive property (2.7 folds) and intestinal permeation (~1.8-fold) higher than IPI vesicles (F3). There was a significant (p < 0.05) enhancement in size, muco-adhesion, and permeation flux achieved after coating with chitosan. The IPI chitosan vesicle (F3C) demonstrated an enhanced bleeding time of 525.33 ± 12.43 s, anti-thrombin activity of 59.72 ± 4.21, and inhibition of platelet aggregation 68.64 ± 3.99%, and anti-platelet activity of 99.47%. The results of the study suggest that IPI chitosan vesicles showed promising in vitro results, as well as improved anti-platelet and anti-thrombotic activity compared to pure IPI and IPI vesicles. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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17 pages, 7558 KiB  
Article
Development, In-Vitro Characterization and Preclinical Evaluation of Esomeprazole-Encapsulated Proniosomal Formulation for the Enhancement of Anti-Ulcer Activity
by Dibyalochan Mohanty, Ameeduzzafar Zafar, Mohammed Jafar, Atul Kumar Upadhyay, Mohammad Akiful Haque, Jeetendra Kumar Gupta, Vasudha Bakshi, Mohammed M. Ghoneim, Sultan Alshehri, Mohammed Asadullah Jahangir and Mohammed Javed Ansari
Molecules 2022, 27(9), 2748; https://doi.org/10.3390/molecules27092748 - 25 Apr 2022
Cited by 3 | Viewed by 1854
Abstract
Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs formulation was developed by slurry method and optimized by 33 box-Bhekhen statistical design software. Span 60 (surfactant), cholesterol, EZL concentration were taken [...] Read more.
Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs formulation was developed by slurry method and optimized by 33 box-Bhekhen statistical design software. Span 60 (surfactant), cholesterol, EZL concentration were taken as independent variables and their effects were evaluated on vesicle size (nm), entrapment efficiency (%, EE) and drug release (%, DR). Furthermore, optimized EZL-PNs (EZL-PNs-opt) formulation was evaluated for ex vivo permeation, pharmacokinetic and ulcer protection activity. Result: The EZL-PNs-opt formulation showed 616 ± 13.21 nm of vesicle size, and 81.21 ± 2.35% of EE. EZL-PNs-opt exhibited negative zeta potential and spherical confirmed scanning electron microscopy. EZL-PNs-opt showed sustained release of EZL (95.07 ± 2.10% in 12 h) than pure EZL dispersion. The ex-vivo gut permeation result exhibited a significantly (p < 0.05) enhanced flux than pure EZL. The in vivo results revealed 4.02-fold enhancement in bioavailability and 61.65% protection in ulcer than pure EZL dispersion (43.82%). Conclusion: Our findings revealed that EZL-PNs formulation could be an alternative delivery system of EZL to enhance oral bioavailability and antiulcer activity. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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13 pages, 4751 KiB  
Article
Synthesis, Characterization, and Assessment of Anti-Cancer Potential of ZnO Nanoparticles in an In Vitro Model of Breast Cancer
by Alaa A. A. Aljabali, Mohammad A. Obeid, Hamid A. Bakshi, Walhan Alshaer, Raed M. Ennab, Bahaa Al-Trad, Wesam Al Khateeb, Khalid M. Al-Batayneh, Abdulfattah Al-Kadash, Shrouq Alsotari, Hamdi Nsairat and Murtaza M. Tambuwala
Molecules 2022, 27(6), 1827; https://doi.org/10.3390/molecules27061827 - 11 Mar 2022
Cited by 20 | Viewed by 3226
Abstract
Advanced innovations for combating variants of aggressive breast cancer and overcoming drug resistance are desired. In cancer treatment, ZnO nanoparticles (NPs) have the capacity to specifically and compellingly activate apoptosis of cancer cells. There is also a pressing need to develop innovative anti-cancer [...] Read more.
Advanced innovations for combating variants of aggressive breast cancer and overcoming drug resistance are desired. In cancer treatment, ZnO nanoparticles (NPs) have the capacity to specifically and compellingly activate apoptosis of cancer cells. There is also a pressing need to develop innovative anti-cancer therapeutics, and recent research suggests that ZnO nanoparticles hold great potential. Here, the in vitro chemical effectiveness of ZnO NPs has been tested. Zinc oxide (ZnO) nanoparticles were synthesized using Citrullus colocynthis (L.) Schrad by green methods approach. The generated ZnO was observed to have a hexagonal wurtzite crystal arrangement. The generated nanomaterials were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), UV-visible spectroscopy. The crystallinity of ZnO was reported to be in the range 50–60 nm. The NPs morphology showed a strong absorbance at 374 nm with an estimated gap band of 3.20 eV to 3.32 eV. Microscopy analysis proved the morphology and distribution of the generated nanoparticles to be around 50 nm, with the elemental studies showing the elemental composition of ZnO and further confirming the purity of ZnO NPs. The cytotoxic effect of ZnO NPs was evaluated against wild-type and doxorubicin-resistant MCF-7 and MDA-MB-231 breast cancer cell lines. The results showed the ability of ZnO NPs to inhibit the prefoliation of MCF-7 and MDA-MB-231 prefoliation through the induction of apoptosis without significant differences in both wild-type and resistance to doxorubicin. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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22 pages, 2752 KiB  
Article
Designing Novel Compounds for the Treatment and Management of RET-Positive Non-Small Cell Lung Cancer—Fragment Based Drug Design Strategy
by Priyanka Ramesh and Shanthi Veerappapillai
Molecules 2022, 27(5), 1590; https://doi.org/10.3390/molecules27051590 - 28 Feb 2022
Cited by 4 | Viewed by 2426
Abstract
Rearranged during transfection (RET) is an oncogenic driver receptor that is overexpressed in several cancer types, including non-small cell lung cancer. To date, only multiple kinase inhibitors are widely used to treat RET-positive cancer patients. These inhibitors exhibit high toxicity, less efficacy, and [...] Read more.
Rearranged during transfection (RET) is an oncogenic driver receptor that is overexpressed in several cancer types, including non-small cell lung cancer. To date, only multiple kinase inhibitors are widely used to treat RET-positive cancer patients. These inhibitors exhibit high toxicity, less efficacy, and specificity against RET. The development of drug-resistant mutations in RET protein further deteriorates this situation. Hence, in the present study, we aimed to design novel drug-like compounds using a fragment-based drug designing strategy to overcome these issues. About 18 known inhibitors from diverse chemical classes were fragmented and bred to form novel compounds against RET proteins. The inhibitory activity of the resultant 115 hybrid molecules was evaluated using molecular docking and RF-Score analysis. The binding free energy and chemical reactivity of the compounds were computed using MM-GBSA and density functional theory analysis, respectively. The results from our study revealed that the developed hybrid molecules except for LF21 and LF27 showed higher reactivity and stability than Pralsetinib. Ultimately, the process resulted in three hybrid molecules namely LF1, LF2, and LF88 having potent inhibitory activity against RET proteins. The scrutinized molecules were then subjected to molecular dynamics simulation for 200 ns and MM-PBSA analysis to eliminate a false positive design. The results from our analysis hypothesized that the designed compounds exhibited significant inhibitory activity against multiple RET variants. Thus, these could be considered as potential leads for further experimental studies. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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10 pages, 29281 KiB  
Article
New Supramolecular Drug Carriers: The Study of Organogel Conjugated Gold Nanoparticles
by Joanna Kowalczuk, Andrzej Łapiński, Elżbieta Stolarczyk, Oleg M. Demchuk, Konrad Kubiński, Monika Janeczko, Aleksandra Martyna, Maciej Masłyk and Sylwia Turczyniak-Surdacka
Molecules 2021, 26(24), 7462; https://doi.org/10.3390/molecules26247462 - 09 Dec 2021
Cited by 4 | Viewed by 1933
Abstract
An aqueous solution of sodium citrate stabilized gold nanoparticles (AuNP) in the presence of N-lauroyl-L-alanine (C12ALA) forms a stable gel. The structure of the gel and the distribution profile of AuNP in it were analyzed. Will nanoparticles separated from each [...] Read more.
An aqueous solution of sodium citrate stabilized gold nanoparticles (AuNP) in the presence of N-lauroyl-L-alanine (C12ALA) forms a stable gel. The structure of the gel and the distribution profile of AuNP in it were analyzed. Will nanoparticles separated from each other with sodium citrate behave in the same way in solution and trapped in the gel matrix? Will the spatial limitation of solvent molecules aggregate nanoparticles and destroy their homogeneity? These questions are very important from the point of view of the use of gold nanoparticles, trapped in the gel structure as carriers of drugs in the slow-release process. The lack of homogeneity of this distribution will have a major impact on the rate of release of the appropriate amount of therapeutic drug from the matrix. In this work, we attempt to answer these questions. The performed biological assays revealed that both C12ALA and C12ALA-AuNP show an excellent level of biological neutrality. They might be used as a transporting medium for a drug delivery without affecting the drug’s activity. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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19 pages, 1212 KiB  
Review
Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs
by Arvind Sharma, Kanika Arora, Harapriya Mohapatra, Rakesh K. Sindhu, Madalin Bulzan, Simona Cavalu, Gulsheen Paneshar, Hosam O. Elansary, Ahmed M. El-Sabrout, Eman A. Mahmoud and Abdullah Alaklabi
Molecules 2022, 27(9), 2969; https://doi.org/10.3390/molecules27092969 - 06 May 2022
Cited by 8 | Viewed by 3105
Abstract
At present, the majority of APIs synthesized today remain challenging tasks for formulation development. Many technologies are being utilized or explored for enhancing solubility, such as chemical modification, novel drug delivery systems (microemulsions, nanoparticles, liposomes, etc.), salt formation, and many more. One promising [...] Read more.
At present, the majority of APIs synthesized today remain challenging tasks for formulation development. Many technologies are being utilized or explored for enhancing solubility, such as chemical modification, novel drug delivery systems (microemulsions, nanoparticles, liposomes, etc.), salt formation, and many more. One promising avenue attaining attention presently is supersaturated drug delivery systems. When exposed to gastrointestinal fluids, drug concentration exceeds equilibrium solubility and a supersaturation state is maintained long enough to be absorbed, enhancing bioavailability. In this review, the latest developments in supersaturated drug delivery systems are addressed in depth. Full article
(This article belongs to the Special Issue Drug Discovery and Delivery Systems)
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