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口服给药的挑战以及脂质纳米颗粒作为管理心血管危险因素的有效口服药物载体的应用

Challenges in Oral Drug Delivery and Applications of Lipid Nanoparticles as Potent Oral Drug Carriers for Managing Cardiovascular Risk Factors.

作者信息

Okur Neslihan Ü, Siafaka Panoraia I, Gökçe Evren H

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Health Sciences, Istanbul, Turkey.

Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece.

出版信息

Curr Pharm Biotechnol. 2021;22(7):892-905. doi: 10.2174/1389201021666200804155535.

Abstract

BACKGROUND

The oral application of drugs is the most popular route through which the systemic effect can be achieved. Nevertheless, oral administration is limited by difficulties related to the physicochemical properties of the drug molecule, including low aqueous solubility, instability, low permeability, and rapid metabolism, all of which result in low and irregular oral bioavailability.

OBJECTIVE

The enhancement of oral bioavailability of drug molecules with such properties could lead to extreme complications in drug preparations. Oral lipid-based nanoparticles seem to possess extensive advantages due to their ability to increase the solubility, simplifying intestinal absorption and decrease or eradicate the effect of food on the absorption of low soluble, lipophilic drugs and therefore improving the oral bioavailability.

METHODS

The present review provides a summary of the general theory of lipid-based nanoparticles, their preparation methods, as well as their oral applications. Moreover, oral drug delivery challenges are discussed.

RESULTS

According to this review, the most frequent types of lipid-based nanoparticle, the solid lipid nanoparticles and nanostructured lipid carriers are potent oral carriers due to their ability to penetrate the oral drug adsorption barriers. Moreover, such lipid nanoparticles can be beneficial drug carriers against cardiovascular risk disorders as diabetes, hypertension, etc. Conclusion: In this review, the most current and promising studies involving Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as oral drug carriers are reported aiming to assist researchers who focus their research on lipid-based nanoparticles.

摘要

背景

口服给药是实现全身效应最常用的途径。然而,口服给药受到药物分子物理化学性质相关困难的限制,包括低水溶性、不稳定性、低渗透性和快速代谢,所有这些都会导致口服生物利用度低且不规则。

目的

提高具有此类性质的药物分子的口服生物利用度可能会给药物制剂带来极大的复杂性。基于脂质的口服纳米粒似乎具有广泛的优势,因为它们能够增加溶解度,简化肠道吸收,并降低或消除食物对低溶性、亲脂性药物吸收的影响,从而提高口服生物利用度。

方法

本综述总结了基于脂质的纳米粒的一般理论、其制备方法及其口服应用。此外,还讨论了口服药物递送面临的挑战。

结果

根据本综述,最常见的基于脂质的纳米粒类型,即固体脂质纳米粒和纳米结构脂质载体,由于其穿透口服药物吸附屏障的能力,是有效的口服载体。此外,这种脂质纳米粒可以成为对抗心血管风险疾病如糖尿病、高血压等的有益药物载体。结论:在本综述中,报告了涉及固体脂质纳米粒和纳米结构脂质载体作为口服药物载体的最新且有前景的研究,旨在帮助专注于基于脂质的纳米粒研究的人员。

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