ENHANCED TRANSDERMAL PERMEABILITY OF TELMISARTAN BY A NOVEL NANOEMULSION GEL
Keywords:
Telmisartan, Nanoemulsion gel, Topical delivery, Phase diagramAbstract
Objective: Telmisartan is an angiotensin II type I receptor blocker antihypertensive agent with 42% oral bioavailability. The aim of the present investigation was to develop a nanoemulsion gel to enhance bioavailability of poorly water soluble Telmisartan.
Methods: Different nanoemulsion components (oil, surfactant and co-surfactant) were selected on the basis of solubility and emulsification ability. Pseudotemary phase diagrams were constructed using aqueous titration method. Carbopol 934 was added as a gel matrix to convert nanoemulsion into nanoemulsion gel. Drug loaded nanoemulsions and nanoemulsion gels were characterized for particle size, viscosity, rheological behavior, thermodynamic stability studies and ex vivo permeation studies using rat skin. Transdermal permeation of Telmisartan from nanoemulsion gels was determined using Franz Diffusion cell.
Results: The optimized nanoemulsion gel (NEG) contained Labrafil®M 2125 CS (14.3%) as oil, Acrysol®EL 135 (30.84%) as surfactant, Carbitol® (15.42%) as co-surfactant and (32.44%) water; 20 mg drug and 1% w/w carbopol. The ex vivo permeation profile of optimized formulation was compared to nanoemulsion and normal gel. Permeability parameters like steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) were significantly increased in nanoemulsion (NE) and nanoemulsion gel (NEG) as compared to conventional gel. There was a considerable improvement in bio availability for nanoemulsion gel compared to the conventional telemisartan gel.
Conclusion: Nanoemulsion gel has significantly increased the bio-availability of the drug.
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References
Jaydeep Patel, Garala Kevin, Anjali Patel, Mihir Raval, Navin Sheth. Design and development of a self-nanoemulsifying drug delivery system for telmisartan for oral drug delivery. Int J Pharm Invest 2011;1(1):112-8.
Pouton CW. Lipid formulations for oral administration of drugs: Non-emulsifying, selfÂemulsifying and 'self-microemulsifying'drug delivery systems. Eur J Pharm Sci 2000;11(2):893-8.
RR Lala, NG Awari. Nanoemulsion-based gel formulations of COX-2 inhibitors for enhanced efficacy in inflammatory conditions. Appl Nano Sci 2014;4(2):143-51.
Peltola S, Saarinen-Savolanien P, Kiesvaara J, Suhonen TM, Urtti A. Microemulsion for topical delivery of estradiol. Int J Pharm 2003;254(2):99-107.
Rhee YS, Choi JG, Park ES, Chi SC. Transdermal delivery of ketoprofen using microemulsions. Int J Pharm 2001;228(2):161-70.
Kumar B, Jain SK, Prajapati SK. Effect of penetration enhancer DMSO on in-vitro skin permeation of acyclovir transdermal microemulsion formulation. Int J Drug Delivery 2011;3(1):83-94.
Bhavna Dhawan, Geeta Aggrawal, SL Harikumar. Enhanced transdermal permeability of piroxicam through newel nanoemulgel formulation. Int J Pharm Invent 2014;4(2):64-76.
Madhusudhan B, Rambhau D, Apte SS, Gopinath D. 1-0-alkylglycerol stabilized carbamazepine intravenous o/w nanoemulsions for drug targeting in mice. J Drug Target 2007;15(2):154-61.
Date AA, Nagarsenker MS. Design and evaluation of self nanoemulsified drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm 2007;329(1):166-72.
Sheikh Shafiq, Faiyaz Shakeel, Sushma Talegaonkar, Farhan J Ahmad, Roop K Khar, Mushir Ali. Development and bioavailability assessment of Ramipril nanoemulsion formulation. Eur J Pharm Biopharm 2007;66(2):227-43.
M Jayne Lawrence, Gareth D Rees. Microemulsion-based media as novel drug delivery systems. Adv Drug Delivery Rev 2000;45(1):89-121.
Md Sarfaraz Alam, Md Sajid Ali, Nawazish Alam. Design and characterization of nanostructure topical gel of betamethasone dipropionate for psoriasis. J Appl Pharm Sci 2012;2(10):148-58.
Sandipan Dasgupta. In vitro and in vivo studies on Lomoxicam loaded nanoemulsion gel for topical application. Curr Drug Delivery 2014;11(1):132-8.
Kawakami K, Yoshikawa T, Moroto Uma Y, Kanaoka E, Takahashi K, Nishihara Y, et al. Microemulsion formulation for enhanced absorption of poorly soluble drugs I Prescription design. J Controlled Release 2002;81(1-2):65-74.