Enhanced Transdermal Delivery of Cilnidpine Via Ultradeformable Vesicle Loaded Patch: Statistical Optimization, Characterization and Pharmacokinetic Assessment.

Q2 Pharmacology, Toxicology and Pharmaceutics

Pharmaceutical nanotechnology Pub Date : 2024-11-04 DOI:10.2174/0122117385334963241015164501

D Maheswara Reddy, Mothilal M

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引用次数: 0

Abstract

Objective: The study aimed to address the limitations of oral delivery and enhance the bioavailability of Cilnidipine (often prescribed as antihypertensive drug) (CND) through the development of transdermal patches containing ultra-deformable transferosomes.

Methods: CND, known for its low oral bioavailability and adverse effects, was encapsulated in transferosomes using a thin film hydration method. Seventeen formulations were made (using Box Behnken Design), varying Soya lecithin, Tween-80, and rotary evaporator's speed, and evaluated for vesicle size, polydispersity index (PDI), and entrapment efficiency (EE %). The better formulation was selected based on these parameters and incorporated into transdermal patches. Physicochemical properties, in-vitro and ex-vivo permeation, and skin irritancy studies were conducted on the patches. Pharmacokinetic studies were conducted using male Wistar albino rats.

Results: The study found that the developed transferosomal formulations had vesicle sizes between 185 nm and 401 nm, entrapment efficiency (EE%) between 63% and 92%, and zeta potential ranging from -52 mV to -20 mV. Both in-vitro and ex-vivo permeation studies showed that transferosomal formulations provided significantly better drug permeation than plain Cilnidipine patches, with increased permeation linked to higher PEG-400 concentrations. The transferosomal patches did not cause skin irritation. The optimized formulation exhibited a higher % drug release (85.7±1.5%). In pharmacokinetic studies using male Wistar albino rats, the transferosomal patch CTP-17 demonstrated a higher maximum concentration (Cmax) of 1565.068 mcg/ml and a greater area under the curve (AUC) of 13225.352 μg h/ml compared to oral administration.

Conclusion: The study concludes that the transferosomal patches of CND offer a promising approach for effective transdermal delivery, potentially improving hypertension management for prolonged periods in a controlled manner.

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通过超变形载囊贴片增强西尼平的透皮给药：统计优化、特征描述和药代动力学评估

研究目的该研究旨在通过开发含有超强可变形转运体的透皮贴片，解决口服给药的局限性，并提高西尼地平（通常作为降压药）（CND）的生物利用度：方法：众所周知，CND 的口服生物利用度较低，且存在不良反应，我们采用薄膜水合法将其封装在转运体中。通过改变大豆卵磷脂、吐温-80 和旋转蒸发器的转速，制作了 17 种配方（采用盒式贝肯设计），并对囊泡大小、多分散指数（PDI）和夹带效率（EE %）进行了评估。根据这些参数选出了较好的配方，并将其纳入透皮贴剂中。对这些贴片进行了理化性质、体内外渗透性和皮肤刺激性研究。使用雄性 Wistar 白化大鼠进行了药代动力学研究：研究发现，所开发的转运体制剂的囊泡尺寸介于 185 nm 和 401 nm 之间，夹带效率（EE%）介于 63% 和 92% 之间，zeta 电位介于 -52 mV 和 -20 mV 之间。体外和体内渗透研究表明，转运体制剂的药物渗透性明显优于普通的西尼地平贴片，渗透性的提高与 PEG-400 浓度较高有关。转运体贴片不会对皮肤造成刺激。优化配方的药物释放率更高（85.7±1.5%）。在使用雄性 Wistar 白化大鼠进行的药代动力学研究中，与口服给药相比，转运体贴片 CTP-17 的最大浓度（Cmax）为 1565.068 mcg/ml，曲线下面积（AUC）为 13225.352 μg h/ml：该研究得出结论，CND 的转运体贴片为有效的透皮给药提供了一种前景广阔的方法，有可能以可控的方式改善长期高血压管理。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Pharmaceutical nanotechnology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

4.20

自引率

0.00%

发文量

期刊介绍： Pharmaceutical Nanotechnology publishes original manuscripts, full-length/mini reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.