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生物利用度增强 尼欧索姆技术纲要。

A Compendium of Bioavailability Enhancement Niosome Technology.

机构信息

Department of Pharmaceutics, University Institute of Pharma Sciences, Chandigarh University, Gharuan, Punjab, India.

Department of Pharmacology, Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.

出版信息

Pharm Nanotechnol. 2023;11(4):324-338. doi: 10.2174/2211738511666230309104323.

Abstract

BACKGROUND

Bioavailability is the dissimilarity between the total amount of drug exposure to a person and the actual dose received by his body. The difference in bioavailability between formulations of a given drug can have clinical implications.

METHODS

Poor aqueous solubility, inappropriate partition coefficient, high first-pass metabolism, narrow absorption window, and acidic pH of the stomach are the main reasons behind the low bioavailability of drugs. There are three substantial methods to vanquish these bioavailability issues, namely pharmacokinetic, biological, and pharmaceutical approaches.

RESULTS

In the pharmacokinetic approach a drug molecule is improved by making alterations in its chemical structure. In the biological approach, the course of administration of the drug is changed; for example, if a drug has very less oral bioavailability, it can be injected as parenteral or some other route if feasible. In the pharmaceutical approach to enhance bioavailability, the physiochemical properties of the drug or formulation are modified. It is cost-effective, less time-consuming, and the risk factor is also minimum. Co-solvency, particle size reduction, hydrotrophy, solid dispersion, micellar solubilisation, complexation, and colloidal drug delivery systems are some of the commonly used methods to enhance the dissolution profiles of drugs via the pharmaceutical approach. Similar to liposomes, niosomes are also vesicular carrier systems but non-ionic surfactants are used instead of phospholipids in their formulation, i.e., their bilayer is comprised of non-ionic surfactants that encircle the aqueous compartment. The niosomes are presumed to raise the bioavailability of poorly water-soluble drugs by increasing their uptake by the M cells present in Peyer's patches of lymphatic tissues of the intestine.

CONCLUSION

Niosomal technology has become an attractive method to overcome several limitations due to its various merits like biodegradability, high stability, non-immunogenic nature, low cost, and flexibility to incorporate lipophilic as well as hydrophilic drugs. The bioavailability of many BCS class II and IV drugs has been successfully enhanced using niosomal technology, like Griseofulvin, Paclitaxel, Candesartan Cilexetil, Carvedilol, Clarithromycin, Telmisartan, and Glimepiride. Niosomal technology has also been exploited for brain targeting via nasal delivery for many drugs like Nefopam, Pentamidine, Ondansetron HCl, and Bromocriptine mesylate. Based on this data, it can be concluded that niosomal technology has increased importance in bioavailability enhancement and improving the overall performance of molecules in vitro and in vivo. Thus, niosomal technology holds tremendous potential for scale-up applications, overcoming the drawbacks of conventional dosage forms.

摘要

背景

生物利用度是指一个人所接触的药物总量与他实际从体内吸收的药物剂量之间的差异。同一药物的不同制剂之间的生物利用度差异可能具有临床意义。

方法

药物生物利用度低的主要原因有:水溶性差、分配系数不当、首过代谢高、吸收窗窄、胃酸性 pH 值低。有三种主要方法可以克服这些生物利用度问题,即药代动力学、生物学和药物学方法。

结果

在药代动力学方法中,通过改变药物分子的化学结构来改善药物分子。在生物学方法中,改变药物的给药途径;例如,如果一种药物口服生物利用度很低,可以通过注射或其他可行的途径给予。在药物学方法中,通过改变药物或制剂的物理化学性质来提高生物利用度。这种方法具有成本效益高、耗时少、风险因素低等优点。增溶、减小粒径、水化、固体分散、胶束增溶、络合和胶体药物递送系统是通过药物学方法提高药物溶解特性的常用方法。类似于脂质体,囊泡也是一种囊泡载体系统,但在其配方中使用非离子表面活性剂代替磷脂,即它们的双层由非离子表面活性剂组成,包围水相。囊泡被认为可以通过增加肠内淋巴组织派尔集合淋巴结中 M 细胞的摄取,提高亲水性差的药物的生物利用度。

结论

由于具有生物降解性、高稳定性、非免疫原性、低成本和灵活性,可以包含亲脂性和亲水性药物等优点,因此,囊泡技术已成为克服多种局限性的一种有吸引力的方法。许多 BCS 类 II 类和 IV 类药物的生物利用度已经通过囊泡技术得到了成功提高,如灰黄霉素、紫杉醇、坎地沙坦西酯、卡维地洛、克拉霉素、替米沙坦和格列美脲。囊泡技术还通过鼻内给药用于许多药物的脑靶向,如奈福泮、喷他脒、盐酸昂丹司琼和甲磺酸溴隐亭。基于这些数据,可以得出结论,囊泡技术在提高生物利用度和改善体内外分子的整体性能方面具有重要意义。因此,囊泡技术具有巨大的扩大应用潜力,可以克服传统剂型的缺点。

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