Preparation and statistical optimization of self nanoemulsifying tablets of Efavirenz using 23 factorial designs
Keywords:
Self nanoemulsifying drug delivery system, 23 factorial designs and bioavailabilityAbstract
The objective of the present research was to enhance the solubility of poorly water soluble antiretroviral drug i.e. efavirenz, by self nanoemulsifying drug delivery system (SNEDDS) and formulating it as tablets using 23 factorial designs. The SNEDDS were prepared using labrafac PG (15%) as oil, Tween 80 (19%) as surfactant and PEG 200 (38%) as co surfactant that yields the globule size of 142.7nm. The liquid SNEDDS were adsorbed onto aerosil which acts as carrier. The SEM of S-SNEDDS appeared as smooth-surfaced particles without any crystalline shape, indicating complete adsorption of SNEDDS. The absence of drug peak in S-SNEDDS thermogram was attributable to presence of drug in molecularly dissolved state in the vicinity of the lipid excipients. The 23 factorial designs were employed to optimize the concentration of Micro crystalline cellulose, PVP and sodium starch glycollate. The observed values were in close agreement with the predicted values thereby validating the feasibility of the optimization procedure in developing self nanoemulsifying tablets. The relative bioavailability of the S SNEDDS and pure drug were 388.49% and 95.39%, respectively. This confirms that the solubility of the drug has been increased leading to increase in the bioavailability of efavirenz.
References
Kumari G, Singh RK. 2012. Highly Active Antiretroviral Therapy for treatment of HIV/AIDS patients: Current status and future prospects and the Indian scenario. HIV & AIDS Review 11:5-14.
. Date AA, Shibata A, Goede M, Sanford B, Bruzzo KL, Belshan M, Destache CJ. 2012. Development and evaluation of a thermosensitive vaginal gel containing raltegravir + efavirenz loaded nanoparticles for HIV prophylaxis. Antiviral Research 96:430-436.
. Chiappetta DA, Hocht C, Taira C, Sosnik A. 2011. Oral pharmacokinetics of the anti-HIV efavirenz encapsulated within polymeric micelles. Biomaterials 32:2379-2387.
. Veldkamp AI, Heeswijk RV, Meenhorst PL, Mulder JW, Lange JMA, Beijnen JH, Hoetelmans RMW. 1999. Quantitative determination of efavirenz (DMP 266), a novel non-nucleoside reverse transcriptase inhibitor, in human plasma using isocratic reversed-phase high-performance liquid chromatography with ultraviolet detection. Journal of Chromatography B 734:55-61.
. Kawabata Y, Wada K, Nakatani M, Yamada S, Onoue S. 2011. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int J Pharm 420:1-10.
. Kumar BP, Yunoos M, Chandana N, Habeeb N, Himaja B. 2010. Enhancement of dissolution rate of Efavirenz by solid dispersion technique. J Pharmacy Res 3(12):2840-2842.
. Atef E, Belmonte AA. 2008. Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur J Pharm Sci 35:257-263.
. Dixit RP., Nagarsenker MS. 2008. Self-nanoemulsifying granules of ezetimibe: Design, optimization and evaluation. Eur J Pharm Sci 35:183-192.
. Djuris MMJ, Djekic L, Vasiljevic D, Ibric S. 2012. Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release. Int J Pharm 436:58- 65.
. Late SG, Yu YY, Banga AK. 2009. Effects of disintegration-promoting agent, lubricants and moisture treatment on optimized fast disintegrating tablets. Int J Pharm 365:4-11.
. Husban FA, Perrie Y, Mohammed AR. 2011. Formulation of multiparticulate systems as lyophilised orally disintegrating tablets. Eur J Pharm Biopharm 79:627-634.
. Hiorth M, Liereng L,Reinertsen R, Thob I. Formulation of bioadhesive hexylaminolevulinate pellets intended for photodynamic therapy in the treatment of cervical cancer. 2013. Int J Pharma 441(1-2):544-554.
. Selvam RP, Kulkarni PK, Dixit M. 2013. Preparation and evaluation of self-nanoemulsifying formulation of efavirenz. ind j pharm edu res 47(1):47-54.
. Kang JH, Oh DH, Oh YK, Yong CS, Choi HG. 2012. Effects of solid carriers on the crystalline properties, dissolution and bioavailability of flurbiprofen in solid self-nanoemulsifying drug delivery system (solid SNEDDS). Eur J Pharma Biopharm 80:289-97.
. Zhang J, Gao Y, Qian S, Liu X, Zu H. 2011. Physicochemical and pharmacokinetic characterization of a spray-dried malotilate emulsion. Int J Pharm 414:186-192
. Beg S, Jena SS, Patra SN, Rizwan M, Swaina S, Sruti J, Rao MEB, Singh B. 2013. Development of solid self-nanoemulsifying granules (SSNEGs) of ondansetron hydrochloride with enhanced bioavailability potential. Colloids and Surfaces B: Biointerfaces 101:414-23.
. Malakara J, Nayak AK. 2012. Formulation and statistical optimization of multiple-unit ibuprofen-loaded buoyant system using 23-factorial design. Chem Eng Res and Design 90(11):1834-1846.
. Singh G, Pai RS, Devi VK. 2012. Response surface methodology and process optimization of sustained release pellets using taguchi orthogonal array design and central composite design. J Adv Pharm Tech Res 3(1):30-40.
. Swamy PV, Shahidulla SM, Shirsand SB, Hiremath SN, Ali MD. 2008. Orodispersible tablets of carbamazepine prepared by direct compression method using 32 full factorial design. Dhaka Univ J Pharm Sci 7(1):1-5.
. Madgulkar AR, Bhalekar MR, Kolhe VJ, Kenjale YD. 2009. Formulation and optimization of sustained release tablets of venlafaxine resinates using response surface methodology. Indian J Pharm Sci 71 (4):387-394.
. King’ori LD, Walker RB. 2012. The use of response surface methodology to evaluate the impact of level 2 SUPAC-IR changes on the in vitro release of metronidazole and ranitidine from a fixed-dose combination tablet. Dissolution Technologies 28-36.
. Bayrak Z, Tas C, Tasdemir U, Erol H, Ozkan CK, Savaser A, Ozkan Y. 2011. Formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers: In vitro and in vivo evaluation. Eur J Pharm Biopharm 78:499-505
. Bhagwat DA, D’Souza DI. 2012. Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier. Int Curr Pharma J 1(12):414-9.
. Gryczke A, Schminke S, Maniruzzaman M, Beck J, Douroumis D. 2011. Development and evaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granules prepared by hot melt extrusion Colloids and Surfaces B: Biointerfaces 86:275-284.
. Nazzal S, Nutan M, Palamakula A, Shah R, Zaghloul AA, Khan MA. 2002. Optimization of a self-nanoemulsified tablet dosage form of ubiquinone using response surface methodology: effect of formulation ingredients International Journal of Pharmaceutics 240:103-114.
. Chowdary KPR, Devi GSA. 2012. Preclinical pharmacokinetic evaluation of efavirenz -cyclodextrin - pvp inclusion complexes. Int J Pharm Sci Rev Res 15(1):23-6.
