SOLUBILITY ENHANCEMENT OF LURASIDONE HYDROCHLORIDE BY PREPARING SMEDDS
Keywords:
Lurasidone Hydrochloride, Solubility enhancement, SMEDDS, In-vitro dissolution, Ex-vivo diffusionAbstract
Objective: The objective of the study was to enhance solubility of Lurasidone HCl, an atypical antipsychotic drug, by formulating self-micro emulsifying drug delivery system (SMEDDS) and its characterization.
Methods: Solubility study of Lurasidone hydrochloride (LH) was carried out in various surfactants, co surfactants and oils. Pseudo ternary phase diagrams were constructed to identify the self-micro emulsification region. Screening was done so as to determine the proper combination of components. Based on this, LH SMEDDS were prepared using Cremophor RH40 (surfactant), Soluphor P (co-surfactant) and Capmul MCM (oil). The preconcentrate SMEDDS were evaluated for clarity(visual), precipitation, % transmittance, robustness to dilution, freeze thawing, particle size distribution and zeta potential and adsorbed SMEDDS were evaluated for drug content, flow properties, in-vitro dissolution and ex-vivo diffusion studies.
Results: The optimized LH SMEDDS composed of 14% Cremophor RH40, 68% Soluphor P, 18% Capmul MCM with a particle size of 3.95 µm and zeta potential of more than 50 mV showing 80% dissolution in 60 min.
Conclusion: The results of this study prove that SMEDDS help in improving the solubility, dissolution and bioavailability of lurasidone hydrochloride.
Â
Downloads
References
Yan J. Regulators and clinicians alike struggle with off-label use and safety risks of atypical antipsychotics in young patients. The Tablet 2011;12:1-7.
Loehr VR, Trueba AF, James D. Calvert. Lurasidone for the treatment of schizophrenia: new advance or nothing new? The Tablet 2011;12:7-14.
Mittal A, Yadav M, Choudhary D, Shrivastava B. Enhancement of solubility of lurasidone HCl using solid dispersion technique. Int J Res Ayurveda Pharm 2014;5:632-7.
Khan BA, Bakhsh S, Khan H, Mahmood T, Rasul A. Basics of self micro emulsifying drug delivery system. J Pharm Alternative Med 2012;1:13-20.
Mandal S, Mandal S. Microemulsion drug delivery system: a platform for improving dissolution rate of poorly water soluble drug. Int J Pharm Sci Nanotechnol 2011;3:1214-9.
Borhade V, Nair H, Hegde D. Design and evaluation of self-microemulsifying drug delivery system (SMEDDS) of tacrolimus. AAPS PharmSciTech 2008;9:13-21.
Nawale R, Mehta B. Glibenclamide loaded self-microemulsifying drug delivery (SMEDDS): Development and optimization. Int J Pharm Pharm Sci 2013;5:325-30.
Mahajan H, Shaikh T, Baviskar D, Wagh R. Design and development of solid self-microemulsifying drug delivery system (SMEDDS) of fenofibrate. Int J Pharm Pharm Sci 2011;3:163-5.
Deshmukh A, Nakhat P, Yeole P. Formulation and in-vitro evaluation of self-microemulsifying drug delivery system (SMEDDS) of furosemide. Scholars Res Library 2010;2:94-106.
Bali V, Ali M, Ali J. Nanocarrier for enhanced bioavailability of a cardiovascular agent: In vitro, pharmacodynamic, pharmacokinetic and stability assessment. Int J Pharm 2011;403:46-56.
DH Oh. Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier. Int J Pharm 2011;420:412-8.
Ghosh PK, Majithia RJ, Umrethia ML, Murthgy RSR. Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability. AAPS PharmSciTech 2006;7:77-85.
Reddy SM, Reddy MS, Reddy NS, Reddy OM. Formulation and evaluation of novel lipid based solid self nano emulsifying drug delivery system of repaglinide. Int J Pharm Sci 2014;6:106-10.
Ammar HO, Ghorab MM, Mostafa DM, Ghoneim AM. Self-nanoemulsifying drug delivery system for sertraline hydrochloride: Design, Preparation and Characterisation. Int J Pharm Sci 2014;6:589-95.
Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems. Eur J Pharm Sci 2000;11:S93-8.