Investigating superiority of novel bilosomes over niosomes in the transdermal delivery of diacerein:in vitrocharacterization,ex vivopermeation andin vivoskin deposition study

Abstract

Skin is considered the most accessible organ of the body because of its underlying capillary network. However, stratum corneum (SC), the upper most layer of skin, represents major diffusional barrier for most drugs. Hence, the use of edge activators (EAs) in designing novel elastic vesicles is hypothesized to impart their lipid bilayer with ultra-flexibility to trespass SC by high self-optimizing deformability. To confirm this hypothesis, this work aimed at developing novel bilosomes by modulating conventional niosomal composition using different bile salts as EAs and investigating their superiority over niosomes for transdermal delivery of diacerein (DCN), as model drug. Bilosomes were prepared by thin film hydration (TFH) technique according to full 3.2 factorial design to select the optimal formulation using Design-Expert software. The optimal bilosomes (B6) showed nanosized vesicles (301.65 ± 17.32 nm) and 100.00 ± 0.00 % entrapment efficiency. Ex vivo permeation studies and in vivo evaluation revealed that B6 exhibited superior permeation and drug retention capacity compared to the conventional niosomal formulation and drug suspension. Furthermore, B6 was subjected to in vivo histopathological study using male Wistar rats which ensured its safety for topical application. Overall, the results confirmed the hypothesized superiority of bilosomes over niosomes for enhancing DCN flux across the skin.

Fabrication of novel elastosomes for boosting the transdermal delivery of diacerein: statistical optimization, ex-vivo permeation, in-vivo skin deposition and pharmacokinetic assessment compared to oral formulation

“…These elastic vesicles serve as penetration enhancers that can structurally modify SC by their constituting lipids and deeply penetrate through the skin with minimal risk of vesicular wall rupture compared to conventional niosomes and liposomes (Muzzalupo et al., 2011 ; Kakkar & Kaur, 2013 ). The results of our previous work confirmed the ability of bilosomes to be used as vesicular carriers for enhancing the transdermal drug delivery (Al-Mahallawi et al., 2015 ; Aziz et al., 2018 ). In this article, bilosomes was selected as a nucleus for developing novel elastosomes by modulating bilosomal composition using various types of edge activators (EAs).…”

<p>Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation</p>

“…Hence, vesicles acted as drug carriers which not only softened the intercellular matrix of SC but also penetrated deeply to the target site of dermis where a depot from which the drug can be released was formed. 24 Furthermore, there was no significant difference between the T max of TE14 when compared to drug suspension.…”

“…Moreover, the samples were added nonocclusively into the drug pools. [24][25][26] histopathological study…”

“…The specimens were deparaffinized and stained by H&E stains for histopathological examination using a light microscope (Axiostar Plus; ZEISS, Oberkochen, Germany). 24…”

“…The destruction of animal carcasses was achieved by incineration. [24][25][26] Dermatokinetic parameters such as T max , C max , and AUC 0-10 were determined by employing Kinetica ® 5 software (Thermo Fisher Scientific Inc., Waltham, MA, USA). C max and AUC 0-10 were compared between the two treatments using ANOVA test.…”