Abstract：
In order to improve bioavailability, stability, control release, and target delivery of active pharmaceutical ingredients (APIs), as well as to mask their bitter taste, to increase their efficacy, and to minimize their side effects, a variety of microencapsulation (including nanoencapsulation, particle size <100 nm) technologies have been widely used in the pharmaceutical industry. Commonly used microencapsulation technologies are emulsion, coacervation, extrusion, spray drying, freeze-drying, molecular inclusion, microbubbles and microsponge, fluidized bed coating, supercritical fluid encapsulation, electro spinning/spray, and polymerization. In this review, APIs are categorized by their molecular complexity: small APIs (compounds with low molecular weight, like Aspirin, Ibuprofen, and Cannabidiol), medium APIs (compounds with medium molecular weight like insulin, peptides, and nucleic acids), and living microorganisms (such as probiotics, bacteria, and bacteriophages). This article provides an overview of these microencapsulation technologies including their processes, matrix, and their recent applications in microencapsulation of APIs. Furthermore, the advantages and disadvantages of these common microencapsulation technologies in terms of improving the efficacy of APIs for pharmaceutical treatments are comprehensively analyzed. The objective is to summarize the most recent progresses on microencapsulation of APIs for enhancing their bioavailability, control release, target delivery, masking their bitter taste and stability, and thus increasing their efficacy and minimizing their side effects. At the end, future perspectives on microencapsulation for pharmaceutical applications are highlighted.
摘要：
为了提高生物利用度，稳定性,控制释放,和目标递送活性药物成分(API)，以及掩盖他们的苦味，为了增加它们的功效，并尽量减少它们的副作用，各种微囊化(包括纳米封装，粒径<100nm）技术已广泛用于制药行业。常用的微囊化技术是乳液，凝聚,挤压,喷雾干燥,冷冻干燥,分子包涵，微气泡和微海绵，流化床涂层，超临界流体封装，静电纺丝/喷雾，和聚合。在这次审查中,API按其分子复杂性分类：小API（低分子量化合物，比如阿司匹林,布洛芬,和大麻二酚），中等原料药（中等分子量的化合物，如胰岛素，肽，和核酸)，和活的微生物(如益生菌，细菌,和噬菌体）。本文概述了这些微囊化技术，包括其过程，矩阵,以及它们在原料药微囊化方面的最新应用。此外，综合分析了这些常用微囊化技术在提高药物治疗原料药疗效方面的优缺点。目的是总结微囊化原料药在提高其生物利用度方面的最新进展，控制释放,目标交付，掩盖他们的苦味和稳定性，从而提高其疗效并最大限度地减少其副作用。最后,强调了微囊化药物应用的未来前景。
