Abstract
Ophthalmic formulations are not completely available for eliciting therapeutic action because of various reasons such as rapid tear drainage, blinking of eye, lower residence time and lower cul de sac volume. Ophthalmic formulation gets easily drained off due to eye blinking due to low viscosity. Posaconazole is known to have antifungal efficacy as oral route, however ophthalmic efficacy is not studied. The objective of present work was to develop long retentive posaconazole ophthalmic suspension based on polymer platform system of carbopol 974 P and xanthan gum. This synergistic polymer platform was pre-identified by means of experimental design study. Polymer based formulation helps to retain the drug at the site of action for longer duration and does not get washed away due to eye blinking phenomenon. Sterilization is key parameters for ophthalmic formulation. Different methods of sterilization were studied for posaconazole drug as well as polymer mixture and finished product. The developed formulations were characterized for homogeneity, pH, particle size, viscosity, osmolality, rheology study, mucoadhesive strength, contact angle, assay of posaconazole and benzalkonium chloride, degradation product, polymorphic form evaluation, eye irritation test and pharmacodynamic efficacy study. A stable long retentive posaconazole ophthalmic formulation was developed based on principles of quality by design. The developed formulation can be easily manufactured at bigger scale without need of any sophisticated equipment.
Highlights
Ophthalmic formulations have very less bioavailability as they may not be completely eliciting therapeutic action because of reasons such as rapid tear drainage, blinking of eye, lower residence time of ophthalmic formulation in eye and lower cul-de sac volume [1, 2]
For sterilization of posaconazole degradation product was found to be higher in case of gamma sterilization
Impurities were found to be similar for steam, dry heat & ethylene oxide sterilization
Summary
Ophthalmic formulations have very less bioavailability as they may not be completely eliciting therapeutic action because of reasons such as rapid tear drainage, blinking of eye, lower residence time of ophthalmic formulation in eye and lower cul-de sac volume [1, 2]. Simplest way of increasing bioavailability is by formulating mucoadhesive formulation with help of polymers [3]. Formulation adhesiveness/retention in the eye is the function of viscosity being directly proportional; it plays a major role to extend the drug release by increasing the contact time in eye with help of muco-adhesive forces or by polymer inter-penetrated network (IPN) [4]. Significant synergies were considered for those combinations which have higher viscosities compared to their individual viscosities at lower concentrations. These systems would form more viscous solution which remains in the eye for a longer period of time and enhances the extended release
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