Present invention relates to providing lipidic nanoparticulate formulation and method for preparation of the same for injectable and/or topical administration for ocular application. Particularly, this invention relates to method of preparation of biodegradable lipidic nanoparticles drug delivery system of poorly permeable and poorly soluble drugs including acetazolamide and isoniazid by a simple, cost effective, industrially scalable process of mixing the ingredients in water and autoclaving without the use of organic solvents and tedious techniques such as spray drying and high pressure homogenization. The developed drug delivery system provides nanosized particles with uniform distribution and encloses significant amount of active ingredient allowing its controlled release and high permeation across biological membranes. The present system is capable to encapsulate lipophilic, hydrophilic and amphiphilic drugs. The formulation may also contain a suitable antioxidant, preservative, osmotic agent, cryoprotectant, viscolyser, gelling agent and polymer.
