title: Skin Delivery of EGCG and Silibinin: Potential of Peptide Dendrimers for Enhanced Skin Permeation and Deposition.
abstract: 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 (Q12), 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.
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, 576104, Karnataka State, India.
authors.forename: Pallavi Krishna
authors.initials: PK
authors.lastname: Shetty
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, 576104, Karnataka State, India.
authors.forename: Jyothsna
authors.initials: J
authors.lastname: Manikkath
authors.affiliation: School of Pharmacy, Pharmacy Australia Centre of Excellence (PACE), The University of Queensland, Brisbane, QLD, 4072, Australia.
authors.forename: Karnaker
authors.initials: K
authors.lastname: Tupally
authors.affiliation: School of Pharmacy, Pharmacy Australia Centre of Excellence (PACE), The University of Queensland, Brisbane, QLD, 4072, Australia.
authors.forename: Ganesh
authors.initials: G
authors.lastname: Kokil
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, 576104, Karnataka State, India.
authors.forename: Aswathi R
authors.initials: AR
authors.lastname: Hegde
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, 576104, Karnataka State, India.
authors.forename: Sushil Y
authors.initials: SY
authors.lastname: Raut
authors.affiliation: School of Pharmacy, Pharmacy Australia Centre of Excellence (PACE), The University of Queensland, Brisbane, QLD, 4072, Australia.
authors.forename: Harendra S
authors.initials: HS
authors.lastname: Parekh
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, 576104, Karnataka State, India. ss.mutalik@manipal.edu.
authors.forename: Srinivas
authors.initials: S
authors.lastname: Mutalik
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage*; D002392:Catechin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D050091:Dendrimers / Q000737:chemistry*; D008297:Male; D010455:Peptides / Q000737:chemistry; D010539:Permeability; D051381:Rats; D017208:Rats, Wistar; D000077385:Silybin; D012838:Silymarin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D012869:Skin Absorption
chemical_list: D000975:Antioxidants; D050091:Dendrimers; D010455:Peptides; D012838:Silymarin; D000077385:Silybin; D002392:Catechin; C045651:epigallocatechin gallate
keywords: EGCG; antioxidant; peptide dendrimer; silibinin; skin permeation; transdermal