Development, characterization, and assessment of PLAROsomal vesicular system of curcumin for enhanced stability and therapeutic efficacy

IF 3.4 Q2 PHARMACOLOGY & PHARMACY Future Journal of Pharmaceutical Sciences Pub Date : 2024-11-18 DOI:10.1186/s43094-024-00733-y

Somnath Devidas Bhinge, Sheetal Kamble, Dheeraj Randive, Mangesh Bhutkar, Sameer Nadaf, Abhijit Merekar, Kailas Sonawane, Namdeo Jadhav, Asiya Makandar, Mohd Shahnawaz Khan, Shailendra Gurav

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Abstract

Background

Curcumin (CUR) is a natural polyphenol and one of the key phytoconstituents found in the rhizomes of Curcuma Longa. It exhibits various pharmacological properties, encompassing antioxidant, anticancer effects, antiseptic, and anti-inflammatory, among several others.

A significant drawback of using CUR is its limited bioavailability, which primarily depends on gut microorganisms responsible for converting it into its bioavailable form. Therefore, the contemporary study intended to formulate a novel PLAROsomal vesicular delivery of CUR, i.e., CUR-PLAROsomes employing a design of experiments approach to examine the influence of various process parameters, such as particle size and drug percentage release.

Result

The prepared CUR-PLAROsomes were characterized for their physicochemical properties using various hyphenated tools. The CUR-PLAROsomes exhibited sizes ranging from 40 to 300 nm, and the optimized batch demonstrated a drug entrapment of 86.38 ± 0.22%.

In-vitro anticancer studies were conducted using human colorectal adenocarcinoma cells (COLO320DM) and human breast adenocarcinoma (MCF-7). CUR-PLAROsomes exhibited significant in-vivo anti-inflammatory potential against carrageenan-induced paw edema. CUR-PLAROsomes were more potent against COLO320DM and MCF-7 cell lines, even at lower concentrations, than pure CUR.

Conclusion

Furthermore, based on the observations, it exhibits potential as an anti-inflammatory agent, suggesting that PLAROsomes are an effective vesicular drug delivery system.

Highlights

Newly introduced PLARosome is a next generation of Liposomes which have gain popularity owing to its better adaptability to overcome leakage problem of vesicular drug delivery system.
This is the pioneer attempt to prepare Curcumin-loaded PLARosome as an anti-cancer and anti-inflammatory activity.
Nano size of the PLAROsomes may contribute to enhance the efficacy of Curcumin as a target specific drug delivery system.
Site specific delivery of phytoconstituents is possible by use of PLAROsomes as a novel drug delivery system.

Graphical abstract

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开发、鉴定和评估姜黄素的 PLAROsomal 囊泡系统，以提高稳定性和疗效

背景姜黄素（CUR）是一种天然多酚，也是莪术根茎中的主要植物成分之一。它具有多种药理特性，包括抗氧化、抗癌作用、防腐和抗炎等。使用姜黄素的一个显著缺点是其生物利用度有限，这主要取决于负责将其转化为生物利用形式的肠道微生物。因此，本研究打算采用实验设计方法来研究各种工艺参数（如粒度和药物释放百分比）对 CUR-PLAROsomes 的影响，从而配制出一种新型的 CUR PLAROsomal 囊泡递送剂，即 CUR-PLAROsomes。利用人体结直肠腺癌细胞（COLO320DM）和人乳腺腺癌细胞（MCF-7）进行了体外抗癌研究。CUR-PLAROsomes 对卡拉胶诱导的爪水肿具有显著的体内抗炎潜力。CUR-PLAROsomes对 COLO320DM 和 MCF-7 细胞株的抗炎作用比纯 CUR 更强，即使浓度较低也是如此。此外，根据观察结果，PLAROsomes 具有抗炎潜力，表明 PLAROsomes 是一种有效的囊泡给药系统。这是制备具有抗癌和抗炎活性的姜黄素负载 PLARosome 的首次尝试。 PLAROsomes 的纳米尺寸可能有助于提高姜黄素作为靶向给药系统的药效。使用 PLAROsomes 作为新型给药系统，可以实现植物成分的特定部位给药。图表摘要

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来源期刊

Future Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-

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审稿时长

23 weeks

期刊介绍： Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.