含有素的肌体内膜凝用于透皮输送:开发,优化,体外和临床前评估
Ameeduzzafar Zafar1, Mohd Yasir2, Lubhan Singh3
1Department of Pharmaceutics, College of Pharmacy, Jouf University.
Journal of oleo science
|September 1, 2024
概括
这项研究开发了一种新型的通过皮肤输出色素 (LN) 侵入体 (IVM) 凝,以提高其生物可用性和治疗疗效. 优化的LN-IVM凝显示改善了药物释放,透和减少炎症,提供了安全有效的输送系统.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 素 (LN) 是一种具有药理功效的生物活性黄.
- 由于溶解性差和第一通代谢,LN的有限生物可用性阻碍了其治疗用途.
研究的目的:
- 开发和优化通过皮肤输出色素载入的侵入体 (IVM) 凝.
- 通过改善通过皮肤传递来增强LN的治疗疗效.
主要方法:
- 使用2^3的因数设计,准备和优化了LN载荷的侵入体 (IVM).
- 进行了物理化学表征,包括囊泡大小,PDI,EE和zeta潜力.
- 优化的IVM被制成凝,并对粘度,可扩散性,药物释放,活体透,药理动力学和药理动力学进行了评估.
主要成果:
- 优化的LN-IVM显示了可取的物理化学特性 (300.8 nm VS,0.258 PDI,89.92% EE,-18.2 mV zeta潜力) 和球形形态.
- 优化的IVM凝表现出持续的LN释放 (24小时内91.32%,与普通LN凝相比,透流量显著增加 (5.79μg/h/cm2).
- 与口服相比,透皮LN-IVM凝的相对生物可用性增加了2.38倍,脚胀显著减少.
结论:
- 通过皮肤输入的invasomes凝是一种有效和安全的方法,用于输送白素.
- 这种配方显著改善了LN的生物可用性和治疗结果.
- 开发的LN-IVM凝对改善炎症状况的治疗充满了希望.
相关概念视频
01:09Methods for Studying Drug Absorption: In situ
In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
01:27Bioavailability Enhancement: Drug Permeability Enhancement
After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
01:24Modified-Release Drug Delivery Systems: Site-Targeted
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
01:18Transdermal Drug Delivery Systems
Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...