Treatment of Basal Cell Carcinoma Via Binary Ethosomes of Vismodegib: In Vitro and In Vivo Studies

被引：33

作者：

Gamal, Amr F. ^{[1
]}

Sayed, Ossama M. ^{[1
]}

El-Ela, Fatma I. Abo ^{[2
]}

Kharshoum, Rasha M. ^{[1
]}

Salem, Heba F. ^{[1
]}

机构：

[1] Beni Suef Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm, El Shahid Shehata Ahmed Hijaz St, Bani Suwayf, Egypt

[2] Beni Suef Univ, Fac Vet Med, Dept Pharmacol, Bani Suwayf, Egypt

来源：

AAPS PHARMSCITECH | 2020年 / 21卷 / 02期

关键词：

basal cell carcinoma; vismodegib; ethosomes; isopropyl alcohol; histopathology; PERCUTANEOUS PERMEATION; SKIN DELIVERY; CARRIERS; OPTIMIZATION; PENETRATION; FORMULATION; PARAMETERS; LIPOSOMES; NIOSOMES;

D O I：

10.1208/s12249-019-1574-x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Vismodegib (VMD) is a hedgehog inhibitor which indicated for basal cell skin cancer (BCC). This work focuses on investigating the influence of isopropyl alcohol additive for topical delivering and targeting of VMD-loaded binary ethosomes for BCC treatment. Different binary ethosome formulae were prepared based on Box-Behnken design using different concentrations of phospholipid (A), cholesterol (B) and isopropyl alcohol/total alcohol ratio (C). The prepared formulae were characterized for %entrapment efficiency (R-1), vesicle size (R-2), %release (R-3) and steady-state flux (R-4). Increasing A, B and C resulted in significant increase of R-1 and R-2 and significant decrease of R-3 and R-4. The optimization was achieved and the optimum formula was selected to investigate its anti-tumour efficacy in vivo. The optimum formula showed a localized VMD and consequently a significant anti-tumour activity compared with oral VMD. Briefly, VMD-loaded binary ethosome gel could be an effective treatment of BCC with lower side effects. Graphical abstract

引用

页数：11

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