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The formulation and delivery of highly hydrophobic drugs in an optimized dosage form is challenging to formulation scientists. Posaconazole has shown promising action in case studies against fungal keratitis. Biological macromolecules like gellan gum would aid in enhancing the availability of such drugs by increasing the contact time of the formulation. Herein, we propose a transmucosal ocular delivery system of Posaconazole by developing a gellan gum–based in situ gelling nanosuspension. The HPLC method for Posaconazole was developed and validated as per ICH guidelines. The nanosuspension was prepared by microfluidization and optimized by Quality by Design. The gellan gum concentration selected was 0.4% w/v based on the viscosity and mucoadhesion measurements. A greater zone of inhibition of ~ 15 mm was observed for the prepared nanosuspension as compared to ~ 11 mm for the marketed itraconazole nanosuspension. A potential irritancy score of 0.85, considered to be non-irritant, was observed for the developed nanosuspension. Higher drug release of ~ 35% was noted for the nanosuspension compared to about ~ 10% for the coarse suspension. Ex vivo corneal retention studies on excised goat cornea demonstrated ~ 70% drug retention in the tissue. Graphical abstract Graphical abstract depicting the central hypothesis of the work. Supplementary information The online version contains supplementary material available at 10.1007/s13346-022-01155-0.

Symptomatic distresses associated with common ophthalmic infections and their persistence, have remained a tribulation with repeated occurrences. Although being a directly accessible organ, traditional therapeutic strategies exhibiting seemingly fruitful outcome in treatment and prognosis of eye disorders call for improvement in disease intervention. This is due to frequent challenges presented by the ophthalmic environment. Contemporary research has addressed these challenges by applying nanotechnology as a central concept in designing more proficient diagnostic and therapeutic systems for eye ailments. Within such nanosystems (dendrimers, aptamers, metal nanoparticles, etc.), bioactive agents, drugs and genetic materials can be entrapped and these form the key elements that act at the biomolecular stage and bestow a high level of efficacy towards eradication of disease causatives and specificity for recognition and capture aiding diagnostic processes. In the current review, we present researched and patented nanocentric technologies as promising tools in detection and treatment of ophthalmic ailments.

Introduction: Surface engineering of nanocrystals for improving the biopharmaceutical features is a multivariate process involving numerous formulation and process variables, thus making it a complicated process to get the desired biopharmaceutical quality profile. Nano-by-design is hereby proposed as an approach to nanonize an orally active, lipid lowering fenofibrate, to improve feasibility in product development. Methodology: Top-down wet ball milling (media milling) in zirconia planetary chamber was methodically explored for improving the solubility and bioavailability of fenofibrate by formulating a nanosuspension using polyvinyl alcohol as a stabilizer. Several influencing variables were screened using a systematic one-factor-at-a-time approach. DSC, SEM, XRD, and FTIR were utilized for physical characterization of the product during the development stage and study the effect of milling time, milling speed, fenofibrate: stabilizer ratio, premilling time and stabilizer concentration. Potential risk factors affecting critical quality biopharmaceutical attributes of fenofibrate nanocrystals like size, zeta potential, in vitro release, crystallinity and intrinsic solubility were optimized to improve pharmacokinetic performance. Result: Formulated nanosized fenofibrate exhibited a crystalize nature as evident from XRD and DSC, 411 nm size, and a rapid but complete dissolution (~99% in 30 min). This resulted into quick onset of action and improved bioavailability as observed from 51.46% shorter Tmax, 82.63% higher Cmax, and 69.34% higher AUC0–24h, respectively.