Current Nanomedicine - Volume 11, Issue 2, 2021
Volume 11, Issue 2, 2021
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Pharmacosomes: A Versatile Delivery System for Problematic Molecules
Authors: Pulkit Rana, Ayush Mahajan, Dilpreet Singh and Kuldeep SinghAmongst various lipids-based vesicular system, pharmacosomes bear unique advantage over various other lipid based vesicular system. Pharmacosomes are novel vesicular drug delivery system. Pharmacosomes impart better biopharmaceutical properties for synthetic and herbal drugs. Drug incorporated in pharmacosomes encompasses increased bioavailability, reduced toxicity and enhanced stability. Pharmacosome are generally prepared via phospholipid, but various drugs have been derived from different lipid moieties. These include fatty acyl derivatives, fatty alcohol derivative, cholesteryl derivatives. Pharmacosome were evaluated for different parameters such as size, surface morphology, drug entrapment, solubility and in vitro drug release rate. There has been advancement in the scope of this delivery system for several drugs used including NSAIDs, Anti-cancer, anti-viral, anti-hypertension and diuretic drugs. This article reviews the latent pharmacosome as a novel controlled and targeted drug delivery system and highlights the methods of preparation and characterization and application of pharmacosome in drug delivery for herbal and synthetic drugs.
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New Insights into Gastroretentive Dosage Forms in Delivery of Drugs
Authors: Pooja Mathur, Vikas Jhawat and Rohit DuttThe oral drug delivery route is preferable to deliver the therapeutic agents because of the low cost, flexibility in dosage form, and easy administration of drugs responsible for a high range of patient compliance. GRDDS is also an oral route of drug delivery system to prolong gastric residence time, thereby achieving site-specific drug release in the upper GIT for local or systemic effect. Various strategies for developing systematic GRDDS include approaches with less density than stomach contents, systems with high density, swellable and expanding strategies, formulation of super porous hydrogels, gas generating systems, hydrodynamically balanced, raft forming approaches, floating drug delivery, and dual working systems. The massive challenge in developing systemic GRDDS is inter and intra-individual differences in gastric physiology. Despite so many formulation strategies, these systems might be associated with few benefits as well as drawbacks. Drawbacks with few approaches can be overthrown by formulating novel dual working systems such as a Mucoadhesive Floating Drug Delivery System (MFDDS). These systems can form an intimate contact of the formulation with the stomach's mucosal membrane and increase the dosage formulation's absorption at the target site. The present compilation aims to outline the stomach's physiological state, the ideal characteristics of drugs for GRDDS, key factors impacting GRDF efficacy, and gastroretentive formulation strategies that could become the critical processes in the pharmaceutical research for target drug delivery. It also explores various marketed products of GRDDS and future perspectives.
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Acitretin Loaded Nanocarrier Gel: Formulation and Exploration of In-vitro Release Kinetics
Authors: Anupriya Kapoor, Nikunj sethi and Navneet VermaBackground: The present study intended to design and evaluate Acitretin (ACT) loaded Nanostructured Lipid Carriers (NLCs) for the management of psoriasis through topical application. Psoriasis is an autoimmune disorder that affects the skin and is characterized by irritation, red flaky patches over different parts of the body. ACT is an analog of vitamin A that is used for the management of psoriasis via the oral route. The prime demerit associated with oral route delivery of a drug is the teratogenic effect associated with the active molecule and side effects like dry mouth, runny nose, hair loss, taste changes, chapped lips, etc. that are the major contributing factors of reduced patient compliance. Objective: The objective of the present research work was to develop a topical formulation of ACT. Developing topical formulation for the same can result in enhanced patient compliance and can be worth compared to the marketed oral formulation of the drug. Methods: ACT loaded NLCs were prepared by hot homogenization method using oleic acid as a liquid lipid and stearic acid as a solid lipid in a 7:3 ratio along with the combination of a non-ionic surfactant (Tween 80) and an anionic surfactant (sodium lauryl sulphate). Results: In several optimization experiments, formulation F3 was found to be most appropriate for formulating gel. Morphological information obtained from SEM reinforced the formation of particles with nearly spherical morphology. The optimized formulation had a mean diameter of 363 nm, as founded by Zetasizer. XRD studies affirmed that the formulation exhibits amorphous nature, which is an essential character of NLC. An optimized formulation was further incorporated in the gel by using Carbopol 940P as a gelling agent. In vitro release studies indicated 96.85 ± 2% release in 8 hours with Korsmeyer- Peppas model release kinetics. The observed n value1.391 for drug release for F3G2 bespeak Super case II transport may be the result of sorption of the drug from the surface of NLC that is controlled by stress-induced relaxation which occurs at the boundary of the swollen shell. Conclusion: In vitro characterization of ACT (Acitretin) loaded NLC supports the objective that NLC can serve as a potential carrier for topical delivery of ACT and can also reduce oral toxicity associated with drug after stringent evaluation in the near future.
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Preparation and Characterization of 5-Fluorouracil Loaded Nanogels for Skin Cancer Treatments: In Vitro Drug Release, Cytotoxicity and Cellular Uptake Analysis
Authors: Swati Rathore, Vaibhav Rajoriya, Varun Kushwaha, Sanyog Jain and Sushil K. KashawObjective: The present study aimed to explore the in-vitro anticancer potential of 5-fluorouracil (5-FU) loaded PLGA nanogels coated with nerolidol sesquiterpene. Methods: The emulsification-solvent evaporation technique was used for the preparation of plain PLGA nanogels (PNGs) and 5-FU loaded PLGA nanogels (FPNGs). A surface coating of Nerolidol (2%) sesquiterpene was employed to improve the penetration efficacy of the nanogels into the stratum corneum. Results: The nanogels formulation FPNGs have the size range 220±0.25% nm obtained by dynamic light scattering. The entrapment efficiency of approx ˜ 42% with a sustained-release pattern for 24 h was estimated at different pH ranges. The cell uptake and localization profile were revealed by confocal microscopy analysis using the HaCaT cell line. MTT assay demonstrated the cell compatibility of nanogels, confirmed by apoptosis assay depicting the apoptotic index of 0.87. Conclusion: This study concludes that FPNGs are a promising nanogels system against skin cancer that can be used to boost the chemo-therapeutic efficiency of bioactives with sustained and controlled release at the desired site.
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Corrigendum to: Double PEGylation Significantly Improves Pharmacokinetic Properties of Irinotecan Containing Nanoparticles in a Zebrafish Model
Due to an editorial oversight, we would like to apologize for an error that occurred in the print version of an article entitled “Double PEGylation Significantly Improves Pharmacokinetic Properties of Irinotecan Containing Nanoparticles in a Zebrafish Model, 2019, 9(2), 173-181 [1]. It was published as a case report; the article type has been changed to research article now. The original article can be found online at https://doi.org/10.2174/2468187308666180925143701
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