Ion- and pH-activated novel in-situ gel system for... [J Drug Target.

2010] - PubMed result Page 1 of 1

J Drug Target. 2010 Aug;18(7):499-505.

Ion- and pH-activated novel in-situ gel system for sustained ocular
drug delivery.
Gupta H, Velpandian T, Jain S.
Institute of Nuclear Medicine and Allied Sciences, Defence Research and Development Organization, Delhi, India.

Abstract
Poor bioavailability (<1%) of drugs from conventional eye drops is mainly due to the various precorneal loss factors which
include rapid tear turnover, systemic drug absorption through naso-lachrymal duct, transient residence time of the drug
solution in the cul-de-sac and the relative impermeability of the drugs to corneal epithelial membrane. The present study
describes the formulation and evaluation of chitosan and gellan gum based novel in-situ gel system activated by dual
physiological mechanisms. Chitosan (a pH-sensitive polymer) in combination with gellan gum (an ion-activated polymer)
were used as gelling agent. Timolol maleate, the drug which is frequently used for glaucoma therapy was used as model
drug to check the efficacy of the formulation. The developed formulation was characterized for various in vitro parameters,
for example, clarity, gelation pH, isotonicity, sterility, viscosity, transcorneal permeation profile, and ocular irritation. Ocular
retention was studied by gamma scintigraphy and a significant increase in retention time was observed. The formulation
was also found to be nonirritant and well tolerable. The developed system can be a viable alternative to conventional eye
drops for the treatment of various ocular diseases and is suitable for clinical application.

PMID: 20055752 [PubMed - indexed for MEDLINE]

http://www.ncbi.nlm.nih.gov/pubmed/20055752 01-04-2011