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固体脂质纳米粒:提高高溶解性和低渗透性(BCS III类)药物口服生物利用度的潜在选择。

Solid Lipid Nanoparticles: A Potential Option for Enhancing Oral Bioavailability of Highly Soluble and Poorly Permeable (BCS Class III) Drugs.

机构信息

SRM College of Pharmacy, SRMIST, Kattankulathur, Chennai, Tamil Nadu, India.

Department of Pharmacy, SRM College of Pharmacy, SRMIST, Kattankulathur, Chennai, Tamil Nadu, India.

出版信息

Curr Drug Deliv. 2023;20(3):223-236. doi: 10.2174/1567201819666220418100410.

DOI:10.2174/1567201819666220418100410
PMID:35443896
Abstract

Oral administration of drug is the most preferred one among the other routes for the majority of clinical applications. As compared to the parenteral method of administration, it has potential benefits such as increased patient compliance, fewer problems, and reduced treatment costs. Regardless of these factors, inadequate bioavailability owing to poor solubility or permeability limits the therapeutic effectiveness of orally given drugs. Though most current research focuses on BCS II (drugs with low solubility and high permeability), BCS III (drugs with high solubility and low permeability) also has poor oral bioavailability due to their limited permeability across lipid membranes and is usually administered through the parenteral route. The need for an oral alternative to parenteral administration has prompted a renewed focus on the development of innovative dosage forms that support the absorption of medicines that are poorly permeable through the intestinal epithelium. Because of their unique sizedependent feature in enhancing transmembrane permeability, ability to incorporate both lipophilic and hydrophilic drugs and biocompatible nature of components, the use of nanoparticles for improving drug bioavailability has been a focus of current study in the field of drug delivery in recent years. The lipidbased nanoparticle method presents a potential new avenue for manufacturing BCS Class III medicines with enhanced bioavailability, as poor permeability is the main issue for these agents. This research aims to assess the potential of lipid nanoparticles for improving the oral bioavailability of medicines with permeability-restricted oral absorption, such as pharmaceuticals in Biopharmaceutical Classification System (BCS) class III.

摘要

在大多数临床应用中,口服给药是所有给药途径中最受欢迎的一种。与肠胃外给药方法相比,它具有潜在的优势,如患者依从性提高、问题较少以及治疗成本降低。尽管有这些因素,但由于溶解度或渗透性差导致的生物利用度不足限制了口服药物的治疗效果。虽然目前大多数研究集中在BCS II类(低溶解度高渗透性药物),但BCS III类(高溶解度低渗透性药物)由于其跨脂质膜的渗透性有限,口服生物利用度也较差,通常通过肠胃外途径给药。需要一种替代肠胃外给药的口服剂型,这促使人们重新关注开发创新剂型,以支持肠道上皮渗透性差的药物的吸收。由于纳米颗粒在增强跨膜渗透性方面具有独特的尺寸依赖性特征、能够同时包载亲脂性和亲水性药物以及其成分具有生物相容性,近年来,使用纳米颗粒提高药物生物利用度一直是药物递送领域当前研究的重点。基于脂质的纳米颗粒方法为制造具有更高生物利用度的BCS III类药物提供了一条潜在的新途径,因为渗透性差是这些药物的主要问题。本研究旨在评估脂质纳米颗粒提高口服吸收受限的药物(如生物药剂学分类系统(BCS)III类药物)口服生物利用度的潜力。

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