Design and Evaluation of Novel in situ Gel Forming Ocular Drug Delivery System of Kaempferol for Sustain Pharmacological Response against Cataract

Aim

Cataract is an eye disease in which the lens of eyes becomes cloudy. It is a major source of blindness globally. As per the reports published by WHO, around 161 million people are visually compromised worldwide. No clinically proven drug is available to date for the cataract treatment and surgery is the only option left for the management of cataract Treatments other than surgery are just prevention based.

Background

A major setback for the development of ocular medications is the poor bioavailability and low therapeutic response of available conventional ophthalmic solutions in the treatment of cataract due to the instant precorneal removal of the drug. Ophthalmic bioavailability of only 1-10% is generally attained and to overcome this problem frequent installation of the concentrated drug solution is required with increases the systemic absorption of the drug through the nasolacrimal absorption of the drug. The in situ gel forming systems are special drug dosage form that when instilled in the eye as a drop undergoes a transitional change from solution form to the gel with a change in its environmental pH.

Materials and Methods

In the present study, Kaempferol ophthalmic gel was prepared using polymers such as Pectin and HPMC K4M as a pH-triggered gelling system to increase contact time and controlled release, to decrease the rate of administration and upsurge the therapeutic efficacy of the drug. Formulation development involved selection of right polymers from plethora of polymers such as HPMC k4m, Pectin, Carbopol and tween 80 in different compositions. The required quantity of drug (1%) soluble in ethanol was poured onto the polymeric solution and proper mixing was done. To evaluate the efficacy of the formulation developed, various methods were employed-clarity, pH, estimation of gelling capacity, gelling strength, viscosity, in vitro cumulative percent drug release. The composition that satisfies all the above-mentioned parameters, was selected as the optimized formulation and this formulation was used in the pharmacological evaluation of the drug.

Results

The evaluation of the anti-cataract activity of Kaempferol was done by using the sodium selenite-induced cataract model in Wistar rat pups.