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Background  The poor ocular bioavailability of the conventional eye drops is due to lack of corneal permeability, nasolacrimal drainage and metabolic degradation. To overcome this issue, drug encapsulated in mucoadhesive polymer based ocular microspheres have the advantages of improved drug stability, easy administration in liquid form, diffuse rapidly and better ocular tissue internalization.    Methods  The ganciclovir chitosan microspheres (GCM) were prepared by modified water-in-oil emulsification method. The formulation was optimized and characterized by investigating  in vitro  release study, release kinetics, XRD and microspheres stability. Ocular irritancy,  in vivo  ocular pharmacokinetic parameters and histopathology study was evaluated in  Wistar  rats. The use of pharmacokinetic/pharmacodynamic indices and simulation process was carried out to further ensure clinical applicability of the formulation.    Results  The  in vitro  release study showed initial burst (nearly 50 %) in first few minutes and followed Fickian (R 2  = 0.9234, n-value = 0.2329) type of diffusion release mechanism. The XRD and stability studies showed favorable results. The  Wistar  rat eyes treated with GCM showed significant increase in ganciclovir AUC (~4.99-fold) and C max  (2.69-fold) in aqueous humor compared to ganciclovir solution and delay in T max . The C max /MIC 90 , AUC 0–24 /MIC 90 , AUC above MIC 90  and T above MIC 90  were significantly higher in GCM group. The aqueous humor concentration-time profile of ganciclovir in GCM and ganciclovir solution was simulated with every 28.1 and 12.8 h, respectively. The simulated concentration-time profile shows that in duration of 75 h, the ganciclovir solution require six ocular instillations compared to three ocular instillations of the GCM formulation. The photomicrograph of GCM and ganciclovir solution treated rat retina showed normal organization and cytoarchitecture.    Conclusions  Correlating with  in vitro  data, the formulation showed sustained drug release along with improved intraocular bioavailability of ganciclovir in  Wistar  rats.

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Improved intraocular bioavailability of ganciclovir by mucoadhesive polymer based ocular microspheres: development and simulation process in Wistar rats