In-vivo Evaluation and Characterization of Novel In-Situ Gelling System as Controlled Delivery System Containing Ciprofloxacin for Ocular Drug Delivery

Abstract

Objectives: The purpose of this research was to develop the micro emulsion-based in situ gelling systems containing Ciprofloxacin for prophylaxis and treatment of the posterior segment diseases like endophthalmitis.
 Methods: Ciprofloxacin was encapsulated in small droplets owing to form microemulsion, and then the formed droplets were dispersed in a polymer solution that converted into a gel upon triggered by the electrolyte present in the tear fluid.
 Results: The formulation approach provides better absorption, penetration, retention, and improves the bioavailability of the drug. The average concentration reached into vitreous humor from topical microemulsion in situ gelling formulation was ~0.4 µg/ml, which is far more than the concentration required for therapeutic effect (i.e. >0.047 µg/ml or >MIC90 for S. Epidermidis, a pathogen commonly responsible to cause endophthalmitis).
 Conclusion: Thus, novel micro emulsion-based in situ gelling formulation could be a potential drug delivery system for the treatment of posterior segment diseases like endophthalmitis.
 Keywords: Microemulsion, ciprofloxacin, endophthalmitis, ocular, infection, in situ

Formulation and Characterization of pH-Dependent In Situ Gelling System for Ocular Drug Delivery of Ciprofloxacin Hydrochloride and Olopatadine Hydrochloride

“…Existing studies developed several ISG formulations using single CFH and OLH for various eye disorders. In literature, different polymers are implemented to establish formulations, such as sodium alginate, chitosan, Hydroxypropyl Methylcellulose (HPMC), Carbapol-980 (CBL-980), and poloxamers [23][24][25] . Single drugs with a combination of polymers were previously developed, but neither CFH nor OLH has been formulated yet in conjunction using two polymer combinations [21][22][23][24][25][26] .…”

“…In literature, different polymers are implemented to establish formulations, such as sodium alginate, chitosan, Hydroxypropyl Methylcellulose (HPMC), Carbapol-980 (CBL-980), and poloxamers [23][24][25] . Single drugs with a combination of polymers were previously developed, but neither CFH nor OLH has been formulated yet in conjunction using two polymer combinations [21][22][23][24][25][26] . Additionally, the combination of two drugs is more effective than an individual drug; hence in this present investigation, efforts have been taken to develop an ISG formulation incorporating a pH-dependant polymer such as CBL-980 and viscosity grade Hydroxypropylcellulose (HPC) for the effective administration of the CFH and OLH into the eye for prolonged drug release and increased ocular drug bioavailability.…”