Chitosan based controlled release drug delivery of mycophenolate mofetil loaded in nanocarriers system: synthesis and in-vitro evaluation.

Background: Organ transplantation is an important and critical procedure, which requires the suppression of immunity, and to suppress the immunity, a constant plasma concentration of immunosuppressant is required.Objectives: The said objective can be achieved by formulating a controlled release drug delivery system of the drug. Chitosan (CHT) nanoparticles (NPs) have been revolutionizing the conventional drug delivery system, for the past two decades. The aim of the current research work was to develop and evaluate CHT-based mycophenolate mofetil (MMF) loaded nanoparticles (CHT/MMF-NPs) using different drug to polymer ratios.Methods: The challenge was to entrap a lipophilic drug within NPs by the ionic gelation method of the positively charged CHT, using tripolyphosphate (TPP) as the crosslinking agent. The prepared CHT/MMF-NPs were evaluated for physical and chemical characterizations, including particle size, surface charge, entrapment efficiency (EE), surface morphology by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) for chemical compatibilities, X-ray diffractometry (XRD) and in-vitro dissolution studies.Results: Outcomes of the studies revealed that particles were 260 ± 17 nm in diameter, with the smooth and regular surface. Satisfactory values of EE (99%) have indicated the suitability of selected ingredients and employed methodology. Moreover, FTIR has confirmed the chemical compatibilities of the formulations. In-vitro dissolution studies have indicated diffusion type of controlled and sustained drug release during 24 h, with zero-order, as best fit kinetic model.Conclusion: Conclusively, the successful achievement of objectives has indicated the suitability of excipients and methodology to prepare CHT/MMF-NPs for better therapeutic outcomes.

Solid Lipid Nanoparticles of Mycophenolate Mofetil: An Attempt to Control the Release of an Immunosuppressant.

INTRODUCTION: Organ transplantation is a critically important procedure, which requires immune modulation by using immunosuppressants. Development of nanoparticles is an emerging and beneficial engineering process to increase the dissolution rate of poorly soluble immunosuppressants as well as to provide controlled release for better therapeutic outcomes. METHOD: Currently, the nanoprecipitation method was employed to fabricate ß-cyclodextrin (ßCD) facilitated mycophenolate mofetil (MMF)-loaded solid lipid nanoparticles (SLNPs). The prime objectives of the study included, improvement of the dissolution profile of poorly aqueous soluble drug and controlled release from the SLNs to provide steady state drug concentration. Drug release from the prepared SLNs was assessed in two different media, ie, acidic buffer at pH 1.2 and phosphate buffer at pH 7.2 using USP dissolution apparatus for 12 h, followed by the evaluation of drug release mechanism and pattern by applying kinetic models. RESULTS: Justifiably, in acidic medium, the release was found to be 12% more (68%) in comparison to that in basic medium (56%). However, in both dissolution media, drug release was independent of initial concentration (R2>0.95) with non-Fickian type of diffusion mechanism. The outcomes of the study have exhibited that prepared formulations were in nanosized range (80-170 nm) with a net charge of ±23 charge on their surface. They possessed fairly uniform surface with acceptable polydispersity index (0.23±0.09). Scanning electron microscopy (SEM) analysis illustrated that the nanoparticles had uniform particle size and shape. DISCUSSION: The findings show potential applications of the nanoparticles and the method for the development of SLNPs in controlled release of MMF for better therapeutic outcomes. Conclusively, the prepared SLNPs were well designed in nanosized ranges and justifying the once daily controlled release formulation dose of MMF to enhance patient compliance.