Formulate Lornoxicam Bio Adhesive Microspheres Using Different Polymers by Ionotropic Gelation Method and Emulsion Cross Linking Method: An Integrated Molecular Dynamics Approach

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Himansu Bhusan Samal, Itishree Jogmaya Das, Sabina Yasmin, Moumita Karmakar, Arijit Mondal, Anjan Mondal, Bishal Banerjee, Bishal Sarkar, Sourav Roy, Ravi Rawat, Volkan Eyupoglu, Suddhasattya Dey, Niloy Sarkar
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Abstract

Background

Lornoxicam microspheres are promising for targeted, controlled, or extended drug release, and the incorporation of mucoadhesive properties can significantly enhance bioavailability and absorption. This study focuses on the development of bioadhesive microspheres utilizing the ionotropic gelation and emulsion crosslinking methods.

Purpose

The primary aim of this research is to formulate bioadhesive microspheres of Lornoxicam using Sodium Alginate, Carbopol 934, and Chitosan as polymers, while simultaneously evaluating Lornoxicam’s interactions within Alginate-Carbopol 934 and Chitosan matrices through molecular dynamics simulations.

Methods

Formulations T1 to T4 employed drug-to-polymer ratios of 1:1, 1:2, 1:3, and 1:4 for Sodium Alginate and Carbopol 934, while formulations T5 to T8 utilized the same ratios for Chitosan and glutaraldehyde as the crosslinking agent. Comprehensive assessments were conducted on particle size, drug entrapment efficiency, and dissolution rates. Molecular dynamics simulations were performed to analyze Lornoxicam’s interactions within the polymer matrices.

Results

Formulation T7 emerged as the optimal formulation based on extensive evaluation tests. Molecular dynamics simulations revealed stable RMSD values for Lornoxicam across both matrices, with the Chitosan matrix displaying greater fluctuations. Notably, stronger hydrogen bond interactions were observed in the Chitosan matrix, which corresponded to a marginally higher binding energy than the Alginate-Carbopol 934 matrix.

Conclusion

These findings indicate that Chitosan may significantly enhance the pharmaceutical potential of Lornoxicam as a drug delivery system, highlighting the need for further exploration of its therapeutic applications.

Abstract Image

采用亲离子凝胶法和乳液交联法制备氯诺昔康生物胶黏微球:综合分子动力学方法
氯诺昔康微球有望用于靶向、控制或延长药物释放,其黏附特性可以显著提高生物利用度和吸收。本研究的重点是利用离子化凝胶和乳液交联的方法开发生物胶粘剂微球。目的以海藻酸钠、卡波波尔934和壳聚糖为聚合物制备氯诺昔康生物粘附微球,同时通过分子动力学模拟评价氯诺昔康在海藻酸卡波波尔934和壳聚糖基质中的相互作用。方法剂型T1 ~ T4采用海藻酸钠和卡波泊934的药聚合物比分别为1:1、1:2、1:3和1:4,剂型T5 ~ T8采用壳聚糖和戊二醛作为交联剂。对颗粒大小、药物包封效率和溶出率进行了综合评价。分子动力学模拟分析氯诺昔康在聚合物基质中的相互作用。结果通过广泛的评价试验,优选处方T7。分子动力学模拟显示氯诺昔康在两种基质中的RMSD值稳定,壳聚糖基质的波动较大。值得注意的是,壳聚糖基质中观察到更强的氢键相互作用,其结合能略高于海藻酸盐-卡波波尔934基质。结论壳聚糖可显著增强氯诺昔康作为一种给药系统的药物潜力,值得进一步探索其治疗应用。
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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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