Enhancement Of Solubility And Oral Bioavailability Of Poorly Soluble Drug Valsartan By Novel Solid Self Emulsifying Drug Delivery System
Keywords:
Valsartan, solid SEDDS, particle size, neusilin US2 enhanced oral bioavailabilityAbstract
The main objective of present work was to prepare a solid SEDDS for enhancement of oral bioavailability of Valsartan, poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions and freeze-thaw stability. The optimized SMEDDS (F4) formulation of Valsartan contained Capmul MCM (Oil), Kolliphor HS 15 (Surfactant) and PEG 400 (Co-surfactant). This optimized formulation was converted in to solid SEDDS by adding required quantity of Neusilin US2 as adsorbing agent used for in vitro dissolution and bioavailability assessment. The oral bioavailability of Valsartan from solid SEDDS was 1.6-fold higher compared to that of Valsartan suspension in rats, suggesting a significant increase (p < 0.05) in oral bioavailability of Valsartan from solid SEDDS.
References
. Gursoy RN, Benita S. Self-emulsifying
drug delivery systems for improved oral
delivery of lipophilic drugs. Biomedicine
& Pharmacotherapy. 2004; 58: 173-182.
. Tang BC, Jian C G, Xu C H.
Development of solid self-emulsifying
drug delivery systems: preparation
techniques and dosage forms. Drug
Discovery Today. 2008; 5(6): 606-612.
. Patel AR, Vavia PR. (2007). Preparation
and In-Vivo evaluation for SMEDDS
containing fenofibrate. The AAPS
Journal, 2007; 9(3): 344-351.
. Tushar Gadkari T, Chandrachood P,
Ruikar A, Deshpande N, Salvekar J,
Somawane S. Validated stability
indicating LC-PDA-MS method to
investigate pH rate profile and
degradation kinetics of Efavirenz and
identification of hydrolysis product by
LCMS. International journal of pharmacy
and pharmaceutical sciences. 2010; 2:
-176.
. Ladak N, Thompson J. Anaesth.
Intensive Care Med. 2009; 10: 392ă
. Shailesh T. Prajapati Harsh A, Joshi
Chhaganbhai N. Patel. (2013).,
Preparation and Characterization of
Self-Micro emulsifying Drug Delivery
System of Olmesartan medoxomil for
Bioavailability Improvement., Journal of
Pharmaceutics. 2013; 2: 01-09.
. Vishvajith A. kamble Deepali M. jagdale,
Vilasrao J. kadam. International Journal
of Pharma and Bio Sciences V1. 2010;
(2).
. Sheikh S, Shakeel F, Talegaonkar S,
Ahmad FJ, Khar RK, Ali M.
Development and bioavailability
assessment of ramipril nanoemulsion
formulation. Eur J Pharm Biopharm.
;66: 227ă243.
. Neha Tyagi, Satheesh Madhav NV.
Formulation and evaluation of
zidovudine nanosuspensions using a
novel bio polymer from the seeds of
buchanania lanzan. Journal of Drug
Delivery & Therapeutics.2013; 3(4): 85-
. Rajinikanth PS, Neo Woei Keat, Sanjay
Garg. Self-nanoemulsifying Drug
Delivery Systems of Valsartan:
Preparation and In-Vitro
Characterization. International Journal of
Drug Delivery. 2012; 4:153-163.
. Kang BK, Lee JS, Chon SK, Jeong SY,
Yuk SH, Khang G, Lee HB, Cho SH,
Development of self micro emulsifying
drug delivery systems (SEDDS) for oral
bioavailability enhancement of
simvastatin in beagle dogs. International
Journal of Pharmaceutics. 2004; 274:
-73.
. Charman SA, Charman WN, Rogge MC,
Wilson TD, Dutko FJ, Pouton CW. Self
emulsifying drug delivery systems:
Formulation and biopharmaceutical
evaluation of an investigational lipophilic
compound. Pharm Res. 1992; 9: 87-93.
. Tao yi, jianglingwan, huibixu, xiangliang
yang. European journal of
pharmaceutics and biopharmaceutics.
; 70:439-444.
. Anand U. Kyatanwar. Solid self
emulsifying drug delivery systems: A
review. Journal of pharmacy research.
; 3(4): 877-882.
. Jessy Shaji, DigambarJadhav. Newer
approaches to self emulsifying drug
delivery system. International journal of
pharmacy and pharmaceutical sciences.
; 2: 37-41.
. Ahmed A. Hussein, Preparation and
Evaluation of Liquid and Solid Self-Micro
emulsifying Drug Delivery System of
Mebendazole. Iraqi J Pharm Sci. 2014;
(1): 89-100.
. Ehab I. Tahaa b, Saleh Al-Saidanb,
Ahmed M. Samyc, Mansoor A. Khana,
Preparation and in vitro characterization
of self-nano emulsified drug delivery
system (SNEDDS) of all-trans-retinol
acetate: International Journal of
Pharmaceutics. 2004; 285:109ă119.
. Eman Atef et al., Formulation and in
vitro and in vivo characterization of a
phenytoin self-emulsifying drug delivery
system. European journal of
pharmaceutical sciences. 2008; 35: 257-
. Singh K, Chaurasiya A, Awasthi A. Oral
bioavailability enhancement of
Exemestane from Self micro emulsifying
drug delivery system (SEDDS). AAPS
Pharm. Sci. Tech. 2009; 10: 906-916.
. Craig DQM. The use of self-emulsifying
systems as a means of improving drug
delivery. B.T. Gattefosse. 1993; 86: 21-
. Samya M. El-Gizawy, Osama H.
Abdelmageed, Mahmoud A. Omar,
Sayed M. Deryea, Ahmed M. AbdelMegied. Development and Validation of
HPLC Method for Simultaneous
Determination of Amlodipine, Valsartan,
Hydrochlorothiazide in Dosage Form
and Spiked Human Plasma. American
Journal of Analytical Chemistry. 2012; 3:
-430.
. Mohan G, Ramesh B, Kishan V.
Development of sustained release
floating drug delivery system for
norfloxacin: In vitro and in vivo
evaluation. PDA J Pharm Sci Tech.
; 65(3): 198-206.