Recent Advances in Nano-Scale Delivery System: Formulation Development and Testing

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (20 November 2021) | Viewed by 8230

Special Issue Editor

School of Pharmacy, Curtin Medical School, GPO Box U1987, Perth 6845, Australia
Interests: nanomedicine; cancer; diabetes; drug delivery; cell biology; bone
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The field of nanomedicine has undergone several phases of development, and the past 5 years have seen a rampant and promising increase in the types of technologies that have been developed. While numerous labs around the globe conduct research in some form of nanoscale drug delivery system (DDS), not many such DDSs reach the clinical testing stage. This issue aims to cover various aspects of nanoscale DDSs, from design right through to marketing for various ailments. The emphasis is on biological testing, whether it be at the cell culture level, animal testing, or clinical testing. We especially invite articles that cover tests to evaluate the toxicity or perceived toxicity of such DDSs as this is often overlooked in the rush to publish data on novel formulations. We also extend a special invitation to those researchers that have tried to make new nanoscale formulations and have encountered significant issues at any stage from development to clinical testing.

Prof. Dr. Crispin R. Dass
Guest Editor

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Keywords

  • nanomedicine
  • nanoscale drug delivery systems (DDSs)
  • nanoscale DDS formulation techniques
  • pharmacokinetics of promising nanoscale DDSs
  • novel nanoscale DDSs
  • clinically used nanoscale DDSs

Published Papers (3 papers)

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Research

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18 pages, 5285 KiB  
Article
Piceatannol-Loaded Bilosome-Stabilized Zein Protein Exhibits Enhanced Cytostatic and Apoptotic Activities in Lung Cancer Cells
by Nabil A. Alhakamy, Giuseppe Caruso, Mohammed W. Al-Rabia, Shaimaa M. Badr-Eldin, Hibah M. Aldawsari, Hani Z. Asfour, Samah Alshehri, Sami H. Alzaharani, Meshari M. Alhamdan, Waleed Y. Rizg and Ahmed N. Allam
Pharmaceutics 2021, 13(5), 638; https://doi.org/10.3390/pharmaceutics13050638 - 29 Apr 2021
Cited by 14 | Viewed by 2217
Abstract
Piceatannol (PIC) is a naturally occurring polyphenolic stilbene, and it has pleiotropic pharmacological properties. Moreover, PIC has cytotoxic actions among various cancer cells. In this work, preparations of PIC-loaded bilosome–zein (PIC-BZ) were designed, formulated, and characterized, and the optimized PIC-BZ cytotoxic activities, measured [...] Read more.
Piceatannol (PIC) is a naturally occurring polyphenolic stilbene, and it has pleiotropic pharmacological properties. Moreover, PIC has cytotoxic actions among various cancer cells. In this work, preparations of PIC-loaded bilosome–zein (PIC-BZ) were designed, formulated, and characterized, and the optimized PIC-BZ cytotoxic activities, measured as half maximal inhibitory concentration (IC50), against lung cancer cell line was investigated. Box–Behnken design was utilized in order to examine the effect of preparation factors on drug entrapment and particle size. PIC-BZ showed a spherical shape after optimization, and its particle size was determined as 157.45 ± 1.62 nm. Moreover, the efficiency of drug entrapment was found as 93.14 ± 2.15%. The cytotoxic activity evaluation revealed that the adjusted formulation, which is PIC-BZ formula, showed a substantially smaller IC50 versus A549 cells. Cell cycle analysis showed accumulation of cells in the G2-M phase. Moreover, it showed in the sub-G1 phase, a rise of cell fraction suggestion apoptotic improving activity. Increased early and late phases of apoptosis were demonstrated by staining of cells with annexin V. Furthermore, the cellular caspase-3 protein expression was significantly raised by PIC-BZ. In addition, the wound healing experiment confirmed the results. To conclude, compared to pure PIC, PIC-BZ demonstrated a higher cell death-inducing activity against A549 cells. Full article
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17 pages, 4511 KiB  
Article
Novel Green Biosynthesis of 5-Fluorouracil Chromium Nanoparticles Using Harpullia pendula Extract for Treatment of Colorectal Cancer
by Mohammed S. Saddik, Mahmoud M. A. Elsayed, Mohamed Salaheldin A. Abdelkader, Mohamed A. El-Mokhtar, Jelan A. Abdel-Aleem, Ahmed M. Abu-Dief, Mostafa F. Al-Hakkani, Hatem S. Farghaly and Heba A. Abou-Taleb
Pharmaceutics 2021, 13(2), 226; https://doi.org/10.3390/pharmaceutics13020226 - 06 Feb 2021
Cited by 44 | Viewed by 3376
Abstract
Colorectal cancer (CRC) is the third highest major cause of morbidity and mortality worldwide. Hence, many strategies and approaches have been widely developed for cancer treatment. This work prepared and evaluated the antitumor activity of 5-Fluorouracil (5-Fu) loaded chromium nanoparticles (5-FuCrNPs). The green [...] Read more.
Colorectal cancer (CRC) is the third highest major cause of morbidity and mortality worldwide. Hence, many strategies and approaches have been widely developed for cancer treatment. This work prepared and evaluated the antitumor activity of 5-Fluorouracil (5-Fu) loaded chromium nanoparticles (5-FuCrNPs). The green biosynthesis approach using Harpullia (H) pendula aqueous extract was used for CrNPs preparation, which was further loaded with 5-Fu. The prepared NPs were characterized for morphology using scanning and transmission electron microscopes (SEM and TEM). The results revealed the formation of uniform, mono-dispersive, and highly stable CrNPs with a mean size of 23 nm. Encapsulation of 5-Fu over CrNPs, with a higher drug loading efficiency, was successful with a mean size of 29 nm being produced. In addition, Fourier transform infrared (FTIR) and X-ray diffraction pattern (XRD) were also used for the investigation. The drug 5-Fu was adsorbed on the surface of biosynthesized CrNPs in order to overcome its clinical resistance and increase its activity against CRC cells. Box–Behnken Design (BBD) and response surface methodology (RSM) were used to characterize and optimize the formulation factors (5-Fu concentration, CrNP weight, and temperature). Furthermore, the antitumor activity of the prepared 5-FuCrNPs was tested against CRC cells (CACO-2). This in vitro antitumor study demonstrated that 5-Fu-loaded CrNPs markedly decreased the IC50 of 5-Fu and exerted more cytotoxicity at nearly all concentrations than 5-Fu alone. In conclusion, 5-FuCrNPs is a promising drug delivery system for the effective treatment of CRC. Full article
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Review

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20 pages, 846 KiB  
Review
Chitosan Nanoparticles in Atherosclerosis—Development to Preclinical Testing
by Pornsak Sriamornsak and Crispin R. Dass
Pharmaceutics 2022, 14(5), 935; https://doi.org/10.3390/pharmaceutics14050935 - 25 Apr 2022
Cited by 4 | Viewed by 2068
Abstract
Chitosan is a natural biopolymer that is present in an abundant supply in sources such as crustacean shells, mushrooms, and insect exoskeletons. It can be used to make a variety of types of drug formulations and is generally safe to use in vivo; [...] Read more.
Chitosan is a natural biopolymer that is present in an abundant supply in sources such as crustacean shells, mushrooms, and insect exoskeletons. It can be used to make a variety of types of drug formulations and is generally safe to use in vivo; plus, it has inherent cholesterol-reducing properties. While an abundance of papers has tested this biopolymer in nanoparticles in cancer and diabetes research, there is a lag of usage, and hence the paucity of information, in the area of cardiovascular research, specifically in atherosclerosis, the topic of this review. This review highlights some of the deficiencies in this niche area of research, examines the range of chitosan nanoparticles that have been researched to date, and proposes several ways forward to advance this field. Nanoparticles used for both diagnostic and therapeutic purposes are reviewed, with a discussion on how these nanoparticles could be better researched in future and what lays ahead as the field potentially moves towards clinical trials in future. Full article
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