In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

Abstract

Abstract. The objective of this study was to develop an ion-activated in situ gelling vehicle for ophthalmic delivery of matrine. The rheological properties of polymer solutions, including Gelrite, alginate, and Gelrite/alginate solution, were evaluated. In addition, the effect of formulation characteristics on in vitro release and in vivo precorneal drug kinetic of matrine was investigated. It was found that the optimum concentration of Gelrite solution for the in situ gel-forming delivery systems was 0.3% (w/w) and that for alginate solution was 1.4% (w/w). The mixture of 0.2% Gelrite and 0.6% alginate solutions showed a significant enhancement in gel strength at physiological condition. On the basis of the in vitro results, the Gelrite formulations of matrine-containing alginate released the drug most slowly. For each tested polymer solution, the concentration of matrine in the precorneal area was higher than that of matrinecontaining simulated tear fluid (STF) almost at each time point (p<0.05). The area under the curve of formulation 16 (0.2%Gelrite/0.6%alginate) was 4.65 times greater than that of containing matrine STF. Both the in vitro release and in vivo pharmacological studies indicated that the Gelrite/alginate solution had the better ability to retain drug than the Gelrite or alginate solutions alone. The tested formulation was found to be almost non-irritant in the ocular irritancy test. The overall results of this study revealed that the Gelrite/alginate mixture can be used as an in situ gelling vehicle to enhance ocular retention.

Stimuli-responsive hydrogels in drug delivery and tissue engineering

“…Balasubramaniam and group developed ion-activated in situ gelling systems for sustained ophthalmic delivery of ciprofloxacin HCl and concluded that the formulated systems provided sustained release of the drug over a period of 8 h in vitro (Sultana et al, 2006). Sultana and co-workers developed an ionactivated, gelrite based in situ ophthalmic gels of pefloxacin mesylate and compared with conventional eye drops and concluded that this system was capable of effective and controlled management of conjunctivitis (Liu et al, 2010). Liu et al in 2010 investigated in situ gelling Gelrite/Alginate formulations as vehicles for ophthalmic delivery and found that the optimum concentration of gelrite solution for in situ gel-forming delivery systems was 0.3% (w/w) and that for alginate solution was 1.4% (w/w; Vodithala et al, 2010).…”

“…Sultana and co-workers developed an ionactivated, gelrite based in situ ophthalmic gels of pefloxacin mesylate and compared with conventional eye drops and concluded that this system was capable of effective and controlled management of conjunctivitis (Liu et al, 2010). Liu et al in 2010 investigated in situ gelling Gelrite/Alginate formulations as vehicles for ophthalmic delivery and found that the optimum concentration of gelrite solution for in situ gel-forming delivery systems was 0.3% (w/w) and that for alginate solution was 1.4% (w/w; Vodithala et al, 2010). The (mixture of 0.2% Gelrite and 0.6% alginate) solution showed a significant enhancement in gel strength at physiological condition.…”

Bacterial Polysaccharides: Production and Applications in Cosmetic Industry

“…Gellan gum was considered noncarcinogenic based on studies with mice and rats fed with the polysaccharide (0-5 g/kg body weight), wherein no neoplastic or nonneoplastic lesions were observed (Bergfeld et al 2012). Gellan gum (0.2-0.8 %) was also considered as nonirritant to the eyes of rabbits (Liu et al 2010;Ramaiah et al 2007). …”

Polysaccharides as Excipients for Ocular Topical Formulations

“…Such a gelled mixture released in vitro the anticancer drug matrine most slowly. When the solution of this mixture was instilled in rabbit eyes the in situ gelling significantly prolonged drug residence in the precorneal area over the time allowed by the GG or NaAA solution alone (Liu et al, 2010). A further in situ gel-forming polysaccharide mixture is composed of Ch and GG.…”