细二氧化硅作为非晶固体分散载体在增强药物负荷和防止再结晶中的作用综述。

IF 2.8 4区 医学 Q2 PHARMACOLOGY & PHARMACY Current drug delivery Pub Date : 2023-01-01 DOI:10.2174/1567201819666220721111852
Rishab Trivedi, Bappaditya Chatterjee, Sana Kalave, Mrugank Pandya
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引用次数: 0

摘要

无定形固体分散体(ASD)是一个流行的概念,以提高溶解性和口服生物利用度的低水溶性药物。ASD面临两个主要挑战:低药物负荷和储存时的再结晶。几种聚合物载体被用于制造具有高药物负荷的稳定的ASD制剂。二氧化硅在这方面的作用已被证明是重要的。不同类型的二氧化硅,多孔和非多孔,已被用于发展ASD。无定形药物被困在硅孔中或吸附在其表面。由于高孔隙率和宽表面积,二氧化硅提供了更好的药物溶解和高载药量。由于与表面硅烷醇基团的氢键作用,非晶态药物的再结晶受到精细孔隙内有限分子能力的抑制。已经发表了一些关于硅基ASD的研究,其中使用了多种类型的二氧化硅。然而,不同种类的二氧化硅对产品稳定性和载药量的影响很少被研究。本研究分析了多种多孔和非多孔二氧化硅类型及其在发展稳定的ASD中的独特作用。重点介绍了制药工业中常用的各种类型的二氧化硅。
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Role of Fine Silica as Amorphous Solid Dispersion Carriers for Enhancing Drug Load and Preventing Recrystallization- A Comprehensive Review.

Amorphous solid dispersion (ASD) is a popular concept for improving the dissolution and oral bioavailability of poorly water-soluble drugs. ASD faces two primary challenges of low drug loading and recrystallization upon storage. Several polymeric carriers are used to fabricate a stable ASD formulation with a high drug load. The role of silica in this context has been proven significant. Different types of silica, porous and nonporous, have been used to develop ASD. Amorphous drugs get entrapped into silica pores or adsorbed on their surface. Due to high porosity and wide surface area, silica provides better drug dissolution and high drug loading. Recrystallization of amorphous drugs is inhibited by limited molecular ability inside the delicate pores due to hydrogen bonding with the surface silanol groups. A handful of researches have been published on silica-based ASD, where versatile types of silica have been used. However, the effect of different kinds of silica on product stability and drug loading has been rarely addressed. The present study analyzes multiple porous and nonporous silica types and their distinct role in developing a stable ASD. Emphasis has been given to various types of silica which are commonly used in the pharmaceutical industry.

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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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