Formulation and development of self-microemulsifying drug delivery system of pioglitazone
Main Article Content
Abstract
System (BCS) class II drugs. The current research aimed to improve the dissolution of poorly water-soluble antidiabetic
drug pioglitazone HCl by formulating it in SMEDDS. Liquid SMEDDS of pioglitazone HCl were formulated with Capmul
MCM C8 and oleic acid as oil phase, Cremophor RH 40 and Tween 80 as surfactant phase, and Transcutol P as cosurfactant
phase after screening various vehicles. The prepared formulations were evaluated for self-emulsifying ability and phase
diagram was constructed to optimize the system. These systems were further characterized for globule size, effect of pH
and robustness, zeta potential, drug content, viscosity, self-emulsification time, polydispersity index, % transmittance,
thermodynamic stability, surface morphology, and drug release. The system was robust to different pH media and dilution
volumes. The optimized system possessed a mean globule size of 122.2 nm, zeta potential around -22.9 mV, drug content
99.66 ± 0.47%, viscosity 0.8874 ± 0.026 cP, emulsification time 38 s, polydispersity index value of 0.5, and transmittance
value of 99.3 ± 0.6%. Drug release in hydrochloric acid buffer pH 2 was found to be 99.35 ± 0.38%. More than three-fold
increase in dissolution characteristics of pioglitazone HCl in SMEDDS was observed as compared to pure and marketed
formulation. Liquid SMEDDS filled in hard gelatin capsule (HGC) shell was found to be compatible. Stability studies show
there was no sign of phase separation or precipitation and no change in drug content was observed.
Downloads
Article Details
This is an Open Access article distributed under the terms of the Attribution-Noncommercial 4.0 International License [CC BY-NC 4.0], which requires that reusers give credit to the creator. It allows reusers to distribute, remix, adapt, and build upon the material in any medium or format, for noncommercial purposes only.
References
Scientific Discussion, European Medcines Agency. Available from: www.
emeuropeasia.org [Last accessed Dec 2007].
Tang JL, Sun J, He ZG. Self-emulsifying drug delivery systems: Strategy
for improving oral delivery of poorly soluble drugs. Curr Drug Ther
;2:85-93.
Porter CJ, Pouton CW, Cuine JF, Charman WN. Enhancing intestinal drug
solubilisation using lipid-based delivery systems. Adv Drug Deliv Rev
;60:673-91.
Kale AA, Patravale VB. Design and evaluation of self-emulsifying
drug delivery systems (SEDDS) of nimodipine. AAPS Pharm Sci Tech
;9:191-6.
Mahajan HD, Shaikh T, Baviskar D, Wagh RD. Design and development
of solid self-micro-emulsifying drug delivery system (SMEDDS) of
fenofibrate. Int J Pharm Pharm Sci 2011;3:163-6.
Arsen AT, Ogbonna A, Abu-Rmaileh R, Abrahamsson B, Ostergaard J,
Müllertz A. “SNEDDS Containing Poorly Water Soluble Cinnarizine;
Development and in vitro Characterization of Dispersion, Digestion
and Solubilizationâ€. Pharmaceutics 2012;4:641-65.
Date AA, Nagarsenker MS. Design and evaluation of self-nanoemulsifying
drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm
;329:166-72.
Xi J, Chang Q, Chan CK, Meng ZY, Wang GN, Sun JB, et al. Formulation
development and bioavailability evaluation of a self-nanoemulsified
drug delivery system of oleanolic acid. AAPS PharmSciTech
;20:172-82.
Borhade V, Nair H, Hegde D. Design and evaluation of
self-microemulsifying drug delivery system (SMEDDS) of tacrolimus.
AAPS PharmSciTech 2008;9:13-21.
Patel AR, Vavia PR. Preparation and in vivo evaluation of
SMEDDS (Self-microemulsifying drug delivery system) containing
fenofibrate. AAPS J 2007;9:E344-52.
Kamble M, Borwandkar VG, Mane SS, Omkar R. Formulation and
evaluation of lipid based nanoemulsion of glimepiride using
self-emulsifying technology. Indo Am J Pharm Res 2012;2:1011-25.
Sha X, Wu J, Chen Y, Fang X. Self-microemulsifying drug-delivery
system for improved oral bioavailability of probucol: Preparation and
evaluation. Int J Nanomed 2012;7:705-12.
Atef E, Belmonte AA. Formulation and in vitro and in vivo characterization
of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur J
Pharm Sci 2008;35:257-63.
Villar AM, Naveros BC, Campmany AC, Trenchs MA, Rocabert CB,
Bellowa LH. Design and optimization of self-nanoemulsifying drug
delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil.
Int J Pharm 2012;431:161-75.
Syed M. Liquid filled hard gelatin capsule: A modern day approach
to improve bioavailability of class II drugs, Oral Presentation, IIIrd
National Conference on “Recent challenges in pharmaceutical science
and technologyâ€, UICT, Jalgaon, India; 2013.
Tang B, Cheng G, Gu JC, Xu CH. Development of solid self
microemulsifying drug delivery system: Preparation techniques and
dosage forms. Drug Discov Today 2008;13:606-12.
Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of
self-microemulsifying drug delivery system of oridonin. Int J Pharm
;355:269-76.
Sudhanshu S, Preeti KS. Formulation, In vitro characterization and
stability studies of self microemulsifying drug delivery systems of
domperidone. Int J Innov Pharm Res 2010;1:66-73.
Elnaggar YS, El-Massik MA, Abdallah OY. Self-nanoemulsifying drug
delivery systems of tamoxifen citrate: Design and optimization. Int J
Pharm 2009;380:133-41.
Food and Drug Administration. Guidance for industry: Immediate
release solid oral dosage forms: Scale-up and post-approval changes.
Rockville: US Department of Health and Human Services, FDA, Center
for Drug Evaluation and Research; November; Dec 1995.
Grove M, Müllertz A, Nielsen JL. Development and characterisatio n of
self microemulsifying drug delivery systems (SMEDDS) of seocalcitol.
Eur J Pharm Sci 2006;28:233-42.
Bachhav YG, Patravale VB. SMEDDS of glyburide: Formulation, in vitro
evaluation, and stability studies. AAPS Pharm Sci Tech 2009;10:482-7.
ICH Harmonized Tripartite Guideline stability Testing of New drug
Substances and Product Q1A (R2), current step 4 version; Dec 2003.