Thiolated polymers: development and evaluation of transdermal delivery systems for progesterone

Area of Science:

• Polymer chemistry
• Materials science
• Pharmaceutical sciences

Background:

• Transdermal drug delivery systems (TDDS) offer advantages over oral administration, including sustained release and avoidance of first-pass metabolism.
• Development of novel polymeric matrices is crucial for improving the efficacy and patient compliance of TDDS.
• Progesterone, a key hormone, is a candidate for transdermal delivery to manage various gynecological conditions.

Purpose of the Study:

• To synthesize and evaluate polycarbophil-cysteine (PCP-Cys) as a polymeric matrix for transdermal progesterone application.
• To assess the adhesive properties of PCP-Cys compared to existing polymers.
• To investigate the in vitro release and permeation of progesterone from PCP-Cys matrices.

Main Methods:

• Polycarbophil was thiolated via covalent attachment of cysteine to form PCP-Cys.
• Adhesive properties were quantified by measuring the total work of adhesion (TWA) on porcine skin.
• In vitro release and permeation studies were conducted using Franz diffusion cells with porcine skin, and progesterone levels were analyzed by HPLC.

Main Results:

• PCP-Cys films exhibited high cohesive properties due to disulfide bond formation.
• The TWA of PCP-Cys on porcine skin was significantly higher (P <0.05) than control polymers.
• Progesterone permeation through porcine skin was significantly enhanced from PCP-Cys matrices within 24 hours compared to PVP/HPMC and PVP/PVA.

Conclusions:

• PCP-Cys, a partly thiolated polymer, demonstrates potential as a novel matrix for transdermal drug delivery.
• The excellent adhesive properties and enhanced progesterone permeation suggest PCP-Cys is a promising candidate for advanced transdermal formulations.
• Further research into PCP-Cys could lead to improved transdermal progesterone therapies.