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

IF 2.8 4区 医学 Q2 PHARMACOLOGY & PHARMACY
M Sri Rekha, S Sangeetha, A Seetha Devi
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引用次数: 1

摘要

在大多数临床应用中,口服给药是最受欢迎的途径。与肠外给药方法相比,它具有潜在的好处,如增加患者依从性,减少问题和降低治疗费用。不管这些因素,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给药的治疗效果。虽然目前大多数研究集中在BCS II(低溶解度和高通透性的药物),但BCS III(高溶解度和低通透性的药物)由于其通过脂膜的渗透性有限,口服生物利用度也很差,通常通过肠外给药。对口服药物替代肠外给药的需求促使人们重新关注创新剂型的开发,这些剂型支持肠上皮渗透性差的药物的吸收。由于纳米颗粒具有独特的尺寸依赖性,可以增强跨膜渗透性,同时可以结合亲脂性和亲水性药物以及组分的生物相容性,因此利用纳米颗粒提高药物的生物利用度已成为近年来药物传递领域的研究热点。脂基纳米颗粒方法为制造具有增强生物利用度的BCS III类药物提供了一种潜在的新途径,因为这些药物的主要问题是渗透性差。本研究旨在评估脂质纳米颗粒在改善口服吸收受透性限制的药物的口服生物利用度方面的潜力,例如生物制药分类系统(BCS) III类药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Solid Lipid Nanoparticles: A Potential Option for Enhancing Oral Bioavailability of Highly Soluble and Poorly Permeable (BCS Class III) Drugs.

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.

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来源期刊
Current drug delivery
Current drug delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.10
自引率
4.20%
发文量
170
期刊介绍: Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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