Skin Delivery of EGCG and Silibinin: Potential of Peptide Dendrimers for Enhanced Skin Permeation and Deposition

被引:39
作者
Shetty, Pallavi Krishna [1 ]
Manikkath, Jyothsna [1 ]
Tupally, Karnaker [2 ]
Kokil, Ganesh [2 ]
Hegde, Aswathi R. [1 ]
Raut, Sushil Y. [1 ]
Parekh, Harendra S. [2 ]
Mutalik, Srinivas [1 ]
机构
[1] Manipal Univ, Dept Pharmaceut, Manipal Coll Pharmaceut Sci, Manipal 576104, Karnataka, India
[2] Univ Queensland, PACE, Sch Pharm, Brisbane, Qld 4072, Australia
来源
AAPS PHARMSCITECH | 2017年 / 18卷 / 06期
关键词
antioxidant; EGCG; peptide dendrimer; silibinin; skin permeation; transdermal; SOLUBLE DRUG SILYBIN; IN-VITRO RELEASE; TRANSDERMAL DELIVERY; POLY(AMIDOAMINE) DENDRIMERS; PAMAM DENDRIMER; EPIGALLOCATECHIN-3-GALLATE EGCG; PENETRATION ENHANCERS; CHEMICAL ENHANCERS; BIOAVAILABILITY; CATECHINS;
D O I
10.1208/s12249-017-0718-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of the present study was to evaluate the ability of the peptide dendrimers to facilitate transdermal delivery of antioxidants, silibinin, and epigallocatechin-3-gallate (EGCG). Drug-peptide dendrimer complexes were prepared and evaluated for their ability to permeate across the skin. The data revealed the ready formation of complexes between drug and peptide dendrimer in a molar ratio of 1:1. In vitro permeation studies using excised rat skin and drug-peptide dendrimer complexes showed highest values for cumulative drug permeation at the end of 12 h (Q(12)), with corresponding permeability coefficient (Kp) and enhancement ratio values also determined at this time point. With silibinin, 3.96-, 1.81-, and 1.06-fold increase in skin permeation was observed from silibinin-peptide dendrimer complex, simultaneous application of silibinin + peptide dendrimer, and pretreatment of skin with peptide dendrimer, respectively, in comparison with passive diffusion. With EGCG, 9.82-, 2.04-, and 1.72-fold increase in skin permeation was observed from EGCG-peptide dendrimer complex, simultaneous application of EGCG + peptide dendrimer, and pretreatment of skin with peptide dendrimer, respectively, in comparison with passive diffusion. The present study demonstrates the application of peptide dendrimers in effectively delivering antioxidants such as EGCG and silibinin into the skin, thus offering the potential to provide antioxidant effects when delivered via appropriately formulated topical preparations.
引用
收藏
页码:2346 / 2357
页数:12
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