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Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance.
Hamdy Abdelkader1,2, David Wertheim3, Barbara Pierscionek4
1Pharmaceutics Department, Faculty of Pharmacy, Minia University, Minia 61519, Egypt.
Pharmaceutics
|December 2, 2020
Summary
New polymeric inserts offer sustained ocular delivery of curcumin, overcoming its poor solubility and short action time. These in-situ gelling and mucoadhesive inserts improve drug release and corneal permeation for effective eye treatments.
Area of Science:
- Ophthalmic Drug Delivery
- Polymer Science
- Biomaterials
Background:
- Ocular drug delivery faces challenges with long-acting formulations and poor curcumin solubility/stability.
- Conventional eye drops require frequent administration, limiting therapeutic efficacy.
- Curcumin's antioxidant properties are hindered by poor water solubility and stability in suspension.
Purpose of the Study:
- To develop and evaluate polymeric, in-situ gelling, and mucoadhesive inserts for sustained ocular curcumin delivery.
- To overcome limitations of conventional curcumin eye drops.
- To assess the physicochemical, in vitro, and in vivo performance of the developed inserts.
Main Methods:
- Solvent casting method using biocompatible polymers (HPMC, CMC, PL 127, PVA) and plasticizers.
- Characterization of inserts for physicochemical properties, mechanical strength, and mucoadhesion.
- In vitro release and transcorneal permeation studies compared to curcumin suspension.
- In vivo evaluation of ocular tolerability and sustained release.
Main Results:
- Curcumin was primarily dispersed in molecular form within smooth, crack-free inserts.
- Selected inserts showed improved mechanical and mucoadhesive properties.
- Significant enhancement in in vitro curcumin release (7.5- to 9-fold) and transcorneal permeation (5.4- to 8.86-fold) was observed.
- Inserts demonstrated good ocular tolerability and sustained release for over two hours.
Conclusions:
- Polymeric in-situ gelling inserts provide a viable alternative for ocular curcumin delivery.
- The developed inserts enhance curcumin's release, permeation, and duration of action.
- This novel formulation overcomes the limitations of conventional eye drops for curcumin.
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