Ashok. P, Meyyanathan. S. N, R. Vadivelan, Jawahar. N
Ashok. P1*, Meyyanathan. S. N1, R. Vadivelan2, Jawahar. N3
1Department of Pharmaceutical Analysis, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Ooty, Nilgiris, Tamil Nadu, India.
2Department of Pharmacology, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Ooty, Nilgiris, Tamil Nadu, India.
3Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Ooty, Nilgiris, Tamil Nadu, India.
Volume - 11,
Issue - 1,
Year - 2021
Nifedipine is a dihydropyridine calcium channel antagonist initially prescribed for treatment of angina pectoris and hypertension. The drug belongs to BCS Class-2 drug, is poorly water soluble drug, it suffers from a poor aqueous solubility, hence the delays its onset of action. Therefore, the purpose of the research study is to adopt the nanotechnology to formulate nanoparticles that improve the rate of dissolution of drug and to get desired bioavailability of nifedipine. Nanosuspensions were prepared by Solid Lipid NanoParticles method in the presence of selected stabilizers at different concentrations. The nanosuspensions were determined for their particle size of drug, zeta potential of drug, drug content and drug dissolution. The selected formula was freeze dried and illustrated by scanning electron microscopy (SEM), FT-IR, differential scanning calorimetry (DSC), and pharmacokinetic study. The in vitro dissolution confirmed the rate of drug release greater compared to the pure drug. The optimum formula has a typical particle size of 225.56±4.65nm and zeta potential of -17.84±2.17 mV. The bioavailability parameters in the rabbits were enhanced by 2 folds when compared with the marketed tablets (Calcigard®). Solid lipid nanoparticles method was successfully employed to produce stable Nifedipine nanosuspension by using the suitable concentration of stabilizer (PVA, Tween 80, PVP and HPMC). From this study, it is concluded that formulation of Nifedipine nanosuspension may be a competent approach that boost the rate of dissolution and hence oral bioavailability of drug.
Cite this article:
Ashok. P, Meyyanathan. S. N, R. Vadivelan, Jawahar. N. Nanosuspensions by Solid Lipid Nanoparticles method for the Formulation and in vitro/in vivo characterization of Nifedipine. Asian J. Res. Pharm. Sci. 2021; 11(1):1-6. doi: 10.5958/2231-5659.2021.00001.1
Barratt GM, 2000. Therapeutic applications of
colloidal drug carriers. Pharm Sci Tech Today, 3,163–169.
Chiba Y, Kohri N, Iseki K, Miyazaki K, 1991.
Improvement of dissolution and bioavailability for mebendazole, an agent for
human echinococcosis, by pre- paring solid dispersion with polyethylene glycol.
Chem Pharm Bull, 39, 2158–2160.
White SR, 2005. Acute dystonic reaction and
the neuroleptic malignant syndrome. J Pharm Practice, 18, 175-83.
Moschwitzer J, Achleitner G, Pomper H, Muller
RH, 2004. Development of an intravenously injectable chemically stable aqueous
omeprazole formulation using nanosuspensions. Eur J Pharm Biopharm, 58, 615-9.
Wongmekiat A, Tozuka Y, Oguchi T, Yamamoto K,
2002. Formation of fine drug particles by co-grinding with cyclodextrin. I. the
use of ßcyclodextrin anhydrate and hydrate. Pharm Res, 19, 1867-72.
Itoh K, Pongpeerapat A, Tozuka Y, Oguchi T,
Yamamoto K, 2003. Nanoparticle formation of poorly water soluble drugs from
ternary ground mixtures with PVP and SDS. Chem Pharm Bull, 51, 171-4.
Keck CM, Muller RH, 2006. Drug nanocrystals
of poorly soluble drugs produced by high-pressure homogenization. Eur J Pharm
Biopharm, 62, 3-16.
Chorny M, Fishbein I, Danenberg HD, Golomb G,
2002. Lipophilic drug loaded nanospheres prepared by na- noprecipitation: effect
of formulation variables on size, drug recovery, and release kinetics. J
Controlled Release, 83, 389-400.
Kumar MP, Rao YM, Apte S, 2008. Formulation
of nanosuspensions of albendazole for oral administration. Curr Nanoscience, 4,
Van Eerdenbrugh B, Vermant J, Martens JA,
Froyen L, Van Humbeeck J, Augustijns P, 2009. A screening study of surface
stabilization during the production of drug nanocrystals. J Pharm Sci, 98,
Merisko-Liversidge E, Sarpotdar P, Bruno J,
Hajj S, Wei L. Peltier N, et al. 1996. Formulation and antitumor activity
evaluation of nanocrystalline suspensions of poorly soluble anticancer drugs.
Pharm Res, 13, 272- 8.
Saindane, 2013.Nanosuspension based in situ
gelling nasal spray of carvedilol: development, in vitro and in vivo
characterization. AAPS Pharm Sci Tech, 14, 189- 99.
Wei L, Yonggang Y, Yongshou T, Xinlan X, Yang
C, Liwei M, et al. 2011.Preparation and in vitro/in vivo evalua- tion of
revaprazan hydrochloride nanosuspension. Int J Pharm, 408, 157–62.