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Solid Lipid Nanoparticles: A Potential Option for Enhancing Oral Bioavailability of Highly Soluble and Poorly Permeable (BCS Class III) Drugs.
Current drug delivery Pub Date : 2023-01-01 , DOI: 10.2174/1567201819666220418100410
Sri Rekha M 1 , Sangeetha S 2 , Seetha Devi A 3
Affiliation  

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.

中文翻译:

固体脂质纳米颗粒: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。

对于大多数临床应用而言,口服给药是其他途径中最优选的一种。与肠胃外给药方法相比,它具有潜在的好处,例如提高患者依从性、减少问题和降低治疗成本。不管这些因素如何,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(低溶解度和高渗透性药物),但 BCS III(高溶解度和低渗透性药物)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. 对口服替代肠胃外给药的需求促使人们重新关注创新剂型的开发,以支持难以通过肠上皮渗透的药物的吸收。由于其在增强跨膜通透性、结合亲脂性和亲水性药物的能力以及组分的生物相容性方面的独特尺寸依赖性特征,近年来利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生物利用度更高的 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。
更新日期:2022-04-18
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