DESIGN AND CHARACTERIZATION OF CANDESARTAN CILEXETIL ORAL NANOEMULSION CONTAINING GARLIC OIL
CANDESARTAN CILEXETIL ORAL NANOEMULSION
Objective: This study was designed to prepare and characterize oil in water (o/w) nanoemulsion of candesartan cilexetil for oral administration. Preparation of candesartan cilexetil as nanoemulsion could increase its water solubility and thus could enhance its bioavailability.
Methods: Aqueous titration method was used to construct the pseudo-ternary phase diagrams of nanoemulsion (NE) consisting of oil, various weight ratios of surfactant and co-surfactant (S mix), and deionized water. Different characterization techniques were conducted on the prepared nanoemulsions to obtain the optimized formula.
Results: Characterizations of formula NE-4 (consists of 0.16% of candesartan cilexetil, 10% of garlic oil, 35 % of S mix (3:1) and 54.84% of deionized water) revealed the following characteristics: droplet size range (95-139 nm), polydispersity index (0.14), zeta potential value (-41.06 mV) and pH value (6.71), which are suitable for oral administration. Candesartan cilexetil in vitro release from this formula was significantly high (P<0.05) and scanning probe microscopy (SPM) study confirmed that the optimized formula (NE-4) was in nano-scale.
Conclusion: Nanoemulsion formula 4 (NE-4) of candesartan cilexetil is the optimized formula and it could be a promising formula for improving the water solubility of candesartan cilaxetil.
2. Darwhekar GN, Jain DK, Chouhan J. Biopharmaceutical classification of candesartan and candesartan cilexetil. Asian J Pharm Life Sci 2012;2:295–302.
3. Jagtap S, Magdum C, Jadge D, Jagtap R. Solubility enhancement technique: a review. J Pharm Sci Res 2018;10:2205–11.
4. Jaiswal M, Dudhe R, Sharma PK. Nanoemulsion: an advanced mode of drug delivery system. Biotechnology 2015;5:123–7.
5. Chouksey R, Jain AK, Pandey H, Maithil A, College GM, Satya S, et al. Development and bioavailability studies of atorvastatin nanoemulsion. Int J Pharm Life Sci 2011;2:982–8.
6. Abo Enin HA. Self-nano emulsifying drug-delivery system for improved oral bioavailability of rosuvastatin using natural oil antihyperlipidemic. Drug Dev Ind Pharm 2015;41:1047–56.
7. Zhang Y, Shang Z, Gao C, Du M, Xu S, Song H, et al. Nanoemulsion for solubilization, stabilization, and in vitro release of pterostilbene for oral delivery. AAPS PharmSciTech 2014;15:1000–8.
8. Mantena AD, Dontamsetti BR, Nerella A. Formulation, optimization and in vitro evaluation of rifampicin nanoemulsions. Int J Pharm Sci Drug Res 2015;7:451–5.
9. Husain A, Mitra MSA, Bhasin PS. A review of the pharmacological and pharmaceutical profile of irbesartan. Pharmacophore 2011;2:276–86.
10. Sisinthy SP, Rao NK, Sarah CYL. Design, optimization and in vitro characterization of self nano emulsifying drug delivery system of olmesartan medoxomil. Int J Pharm Pharm Sci 2016;9:94.
11. Araujo AAS, Bezerra M dos S, Storpirtis S, Matos J do R. Determination of the melting temperature, the heat of fusion, and purity analysis of different samples of zidovudine (AZT) using DSC. Brazilian J Pharm Sci 2010;46:37–43.
12. Poluri K, Sistla RK, Veerareddy PR, Narasu ML. Formulation and preparation of felodipine nanoemulsions. Asian J Pharm Clin Res 2011;4(Suppl 1):116–7.
13. Ghareeb MM, Neamah AJ. Formulation and characterization of nimodipine nanoemulsion as ampoule for oral route. Int J Pharm Sci Res 2017;8:591–602.
14. Chhabra G, Chuttani K, Mishra AK, Pathak K. Design and development of nanoemulsion drug delivery system of amlodipine besilate for improvement of oral bioavailability. Drug Dev Ind Pharm 2011;37:907–16.
15. Chidi E. Development and evaluation of nanoemulsion formulations for improved oral delivery of carvedilol. Univers J Pharm Res 2018;2:5–11.
16. Sharma N, Mishra S, Sharma S, Deshp RDe, Sharma RK. Preparation and optimization of nanoemulsions for targeting drug delivery. Int J Drug Dev Res 2009;5:37-48.
17. Singh KK, Vingkar SK. Formulation, antimalarial activity and biodistribution of oral lipid nanoemulsion of primaquine. Int J Pharm 2008;347:136–43.
18. Khachane PV, Jain AS, Dhawan VV, Joshi GV, Date AA, Mulherkar R, et al. Cationic nanoemulsions as potential carriers for intracellular delivery. Saudi Pharm J 2015;23:188–94.
19. Drais HK, Hussein AA. Formulation and characterization of carvedilol nanoemulsion oral liquid dosage form. Int J Pharm Pharm Sci 2015;7:209–16.
20. Ramakrishna S, Mihira V, Raja Vyshnavi K, Ranjith V. Design and evaluation of drug release kinetics of meloxicam sustained release matrix tablets. Int J Curr Pharm Res 2012;4:90–9.
21. Shakeel F, Haq N, Ali M, Alanazi FK, Alsarra IA. Impact of viscosity and refractive index on droplet size and zeta potential of model O/W and W/O nanoemulsion. Curr Nanosci 2013;9:248–53.
22. Ali HH, Hussein AA. Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies. AAPS Open 2017;3:1-16.
23. Arora R, Aggarwal G, Harikumar SL, Kaur K. Nanoemulsion based hydrogel for enhanced transdermal delivery of ketoprofen. Adv Pharm 2014;1–12. http://dx.doi.org/10.1155/2014/468456
24. Karthikeyan S, Jeeva PA, Jerobin J, Mukherjee A, Chandrasekaran N. Formulation and characterization of nanoemulsion coatings from Azadirachta Indica. Int J ChemTech Res 2012;4:1566–70.
25. Thirupathi A, Meshram S, Sampathi S. Solid state characterization of the polymorphic changes in candesartan cilexetil solid dispersion with polyethylene glycol 8000. Int J Pharm Sci Res 2014;6:27–32.
26. Kamalakkannan V, Puratchikody A, Ramanathan L. Development and characterization of controlled release polar lipid microparticles of candesartan cilexetil by solid dispersion. Res Pharm Sci 2013;8:125–36.
27. Asdaq SM, Inamdar MN. Potential of garlic and its active constituent, S-allyl cysteine, as antihypertensive and cardioprotective in the presence of captopril. Phytomedicine 2010;17:1016–26.
28. Ngan CL, Basri M, Tripathy M, Karjiban RA, Abdul Malek E. Physicochemical characterization and thermodynamic studies of a nanoemulsion-based transdermal delivery system for fullerene. Sci World J 2014. http://dx.doi.org/10.1155/2014/219035
29. Guttoff M, Saberi AH, Mcclements DJ. Formation of vitamin D nanoemulsion-based delivery systems by spontaneous emulsification: factors affecting particle size and stability. Food Chem 2015;171:117–22.
30. Elmarzugi NA. Preparation and evaluation of olive oil nanoemulsion using sucrose monoester. Int J Pharm Pharm Sci 2013;5:434–40.
31. Honary S, Zahir F. Effect of zeta potential on the properties of nano-drug delivery systems-a review (Part 2). Trop J Pharm Res 2013;12:265-73.
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