Formulation, characterization and in vitro-in vivo evaluation of flurbiprofen-loaded nanostructured lipid carriers for transdermal delivery

被引:51
作者
Kawadkar, Jitendra [1 ]
Pathak, Ashwinkumar [1 ]
Kishore, Raj [1 ]
Chauhan, Meenakshi Kanwar [1 ]
机构
[1] Univ Delhi, Delhi Inst Pharmaceut Sci & Res, NDDS Res Lab, Dept Pharmaceut, New Delhi 110017, India
关键词
Nanostructured lipid carriers; flurbiprofen; solubility; transdermal; differential scanning calorimetry; pharmacokinetics; bioavailability; anti-inflammatory; stability; NANOPARTICLES SLN; PHYSICOCHEMICAL PROPERTIES;
D O I
10.3109/03639045.2012.686509
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Flurbiprofen is used in the treatment of arthritis. However, its multiple dosing due to short elimination half life is a concern for such treatment. This work aims to develop nanostructured lipid carriers (NLCs) of flurbiprofen and evaluate their potential for transdermal delivery. The NLCs were prepared by the optimized o/w emulsification-homogenization-sonication technique using coconut oil (liquid lipid). The NLCs were found to be spherical with uniform size (214 nm). The entrapment efficiency and zeta potential were 92.58% and - 30.70 mV, respectively. Differential scanning calorimetry (DSC) showed the amorphous state of flurbiprofen encapsulated in NLCs. The percentage cumulative drug release through the excised rat skin from NLCs was biphasic and significantly prolonged compared with the commercial gel. DSC of the treated skin indicated that the NLCs penetrate into follicles of the skin and accumulate in the dermis. The bioavailability of flurbiprofen from NLCs was more than 1.7-fold that of the commercial gel. The NLCs showed a quick onset and sustained anti-inflammatory effect over period of 24 h for carrageenan-induced rat paw edema than the commercial gel. The stability data revealed that the NLCs were more stable when stored at 5 degrees C. In conclusion, prepared NLCs have potential for skin targeting and sustained drug release.
引用
收藏
页码:569 / 578
页数:10
相关论文
共 25 条
[1]   Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies [J].
Bhaskar, Kesavan ;
Anbu, Jayaraman ;
Ravichandiran, Velayutham ;
Venkateswarlu, Vobalaboina ;
Rao, Yamsani Madhusudan .
LIPIDS IN HEALTH AND DISEASE, 2009, 8
[2]   DYNAMIC LIGHT-SCATTERING STUDY OF INTERNAL MOTIONS OF POLYMER COILS IN DILUTE-SOLUTION [J].
CHU, B ;
WANG, ZL ;
YU, JQ .
MACROMOLECULES, 1991, 24 (26) :6832-6838
[3]   The effect of spray drying solutions of bendroflumethiazide/polyethylene glycol on the physicochemical properties of the resultant materials [J].
Corrigan, DO ;
Healy, AM ;
Corrigan, OI .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 262 (1-2) :125-137
[4]   Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs [J].
Cryer, B ;
Feldman, M .
AMERICAN JOURNAL OF MEDICINE, 1998, 104 (05) :413-421
[5]   Lipid nanoparticles as vehicles for topical psoralen delivery: Solid lipid nanoparticles (SLN) versus nanostructured lipid carriers (NLC) [J].
Fang, Jia-You ;
Fang, Chia-Lang ;
Liu, Chi-Hsien ;
Su, Yu-Han .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2008, 70 (02) :633-640
[6]   Characterization of solidified reverse micellar solutions (SRMS) and production development of SRMS-based nanosuspensions [J].
Friedrich, I ;
Müller-Goymann, CC .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2003, 56 (01) :111-119
[7]  
Han F, 2008, DRUG DEV IND PHARM, V34, P453, DOI [10.1080/03639040701833708, 10.1080/03639040701833708 ]
[8]  
Insel PA., 1996, Goodman and Gilman's The Pharmacological Basis of Therapeutics, P617
[9]   Solid lipid nanoparticles bearing flurbiprofen for transdermal delivery [J].
Jain, SK ;
Chourasia, MK ;
Masuriha, R ;
Soni, V ;
Jain, A ;
Jain, NK ;
Gupta, Y .
DRUG DELIVERY, 2005, 12 (04) :207-215
[10]   Vitamin A loaded solid lipid nanoparticles for topical use:: occlusive properties and drug targeting to the upper skin [J].
Jenning, V ;
Gysler, A ;
Schäfer-Korting, M ;
Gohla, SH .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2000, 49 (03) :211-218