Silk Sericin Functionalized with Carboxy Drugs for Dermocosmetic Applications.
ACS Appl Bio Mater 2026 May 04; 9(9):4091-4101.

Abstract

Silk sericin protein, a textile industry by-product showing no toxicity on oral/topical administration, has recently been exploited as a drug delivery system. The high serine content in sericin makes its functionalization through covalent ester-type bonds feasible; however, only in a few cases have covalent conjugates of sericin with the drug to be delivered been developed. In this paper, we report the preparation of sericin conjugates with carboxy drugs of dermatological interest, i.e., naproxen, retinoic acid, and azelaic acid. Characterization of the purified products by spectroscopic methods, particularly ATR-FTIR, provided evidence for the formation of the ester bond, while SDS-PAGE indicated a substantial modification of the protein. Proteomic analysis allowed the identification of drug-peptide adducts in the samples. The extent of ester functionalization (1-3 w/w%) was estimated by alkaline hydrolysis. No cytotoxicity of NAP@SER on HaCaT was observed over a broad range of concentrations. Ex vivo tests on defatted pig skin demonstrated effective passage of the free drug through the skin (5% w/w of the applied dose) from a NAP@SER glycerol suspension and a significant retention of the drug (33% w/w) within the dermal or epidermal tissues. These results hint at the potential of sericin conjugates as prodrugs for dermal administration.

Authors+Show Affiliations

Argenziano RDepartment of Chemical Sciences, University of Naples "Federico II", Naples 80126, Italy.
Balestrino ADepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Salerno 84084, Italy.
Guillou CUniversity of Rouen Normandie, INSERM US 51, CNRS UAR 2026, HeRacLeS-PISSARO, Normandie Université , Rouen 76000, France.
Nesterenko A0000-0001-8487-1572Université de Technologie de Compiègne, Ecole Supérieure de Chimie Organique et Minérale, Alliance Sorbonne Université, TIMR (Integrated Transformation of Renewable Matter), Compiègne 60200, France.
Panzella L0000-0002-2662-8205Department of Chemical Sciences, University of Naples "Federico II", Naples 80126, Italy.
Lembo SDepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Salerno 84084, Italy.
Hardouin J0000-0003-4588-9811University of Rouen Normandie, INSERM US 51, CNRS UAR 2026, HeRacLeS-PISSARO, Normandie Université , Rouen 76000, France. INSA Rouen Normandie, CNRS, Polymers, Biopolymers, Surfaces Laboratory (UMR 6270), University of Rouen Normandie, Rouen 76000, France.
Guénin E0000-0002-7125-9074Université de Technologie de Compiègne, Ecole Supérieure de Chimie Organique et Minérale, Alliance Sorbonne Université, TIMR (Integrated Transformation of Renewable Matter), Compiègne 60200, France.
Napolitano A0000-0003-0507-5370Department of Chemical Sciences, University of Naples "Federico II", Naples 80126, Italy.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

42011843