Fluorometholone Nanosuspension Case Study

The objective of present study was to prepare a novel stable Fluorometholone ophthalmic Nanosuspension which has advantage over conventional ophthalmic suspension such as blurred vision, burning, stinging and irritation upon instillation. The viscosity was increased to provide additional advantage of long duration of action. Precipitation method was used to prepare Fluorometholone ophthalmic Nanosuspension. The type of polymer and stabilizer used showed effect on the particle size and zeta potential of Fluorometholone. Viscosity of prepared Nanosuspension was carried out which is sufficient to give better retention with cornea. The in-vitro drug release study showed that the optimized Nanosuspension released 98.87% of the drug within 8 hours.
The conventional formulation like solutions, suspension and ointments shows disadvantages such as rapid precorneal elimination, high variability, and drainage by gravity and absence of controlled release. So overcome to these problems newer pharmaceutical ophthalmic formulation such as in-situ gel, Nanoparticle, liposome, Nanosuspension, Microemulsion, Iontophoresis and ocular inserts have been developed in last three decades increase the bioavailability of the drug as a sustained and controlled manner.(1) Fluorometholone is insoluble drug; hence preparation of Nanosuspension can lead to colloidal dispersion having solution like properties with increased retention.(2) Addition of viscosity imparter is an additional advantage. Mainly two types of techniques are available for preparation of Nanosuspension, (1) Bottom up technique (2) Top down technique i.e. High pressure homogenization, lipid emulsion, media milling and dry co-grinding. High pressure homogenization is a reported technique for preparation of Fluorometholone Nanosuspension. The present research work was aimed to develop an optimized formulation & process for Fluorometholone Nanosuspension by Precipitation method. (3, 4, 5)
2. MATERIALS & METHODS
Fluorometholone was a gift-sample from Sentiss pharmaceuticals, Gurgaon, Haryana, India. Hydroxy propyl methyl cellulose E-5 (HPMC E-5), Polyvinyl alcohol was purchased from
4: pH of nanosuspension formulation.
Sr. No. Formulation [Batch no.] PH
1. FF2 7.3± 0.1
The pH value was found to be satisfactory for the ophthalmic formulation and at this pH value the drug will be stable in the formulation as literature survey concludes that Fluorometholone is stable pH 6.2-7.4.
3.3 Specific gravity
Specific gravity bottle was used to check the density of the formulation prepared and in turn compared with the density of water. Weight of empty gravity bottle is taken as (M1), weight of specific gravity bottle containing the preparation is considered as (M2), weight of gravity bottle containing water is taken as (M3). Considering this data we can find Specific gravity bottle is used to check the density of the formulation prepared and in turn compared with the density of water. The optimized batch had the following results.
Weight of preparation: (M2-M1) = (27.0-18.7) =8.3gm/ml
Weight of purified water: (M3-M1) = (26.7-18.7) =8gm/ml
Specific gravity = = 1.037gm
3.4 Particle size measurement
Table no. 5: Particle size of nanosuspension.
Formulation batch Particle size
FF2