Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles (SLNs): Development, characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs?

被引:439
作者
Das, Surajit [1 ]
Ng, Wai Kiong [1 ]
Tan, Reginald B. H. [1 ,2 ]
机构
[1] ASTAR, Inst Chem & Engn Sci, Singapore 627833, Singapore
[2] Natl Univ Singapore, Dept Chem & Biomol Engn, Singapore 117576, Singapore
关键词
Solid lipid nanoparticle; Nanostructured lipid carrier; Clotrimazole; Characterization; Drug release; Stability; DRUG-DELIVERY SYSTEM; PHYSICOCHEMICAL CHARACTERIZATION; BIOAVAILABILITY; FORMULATION; STABILITY; SLN(TM); DESIGN;
D O I
10.1016/j.ejps.2012.05.010
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In recent years, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are among the popular research topics for the delivery of lipophilic drugs. Although SLNs have demonstrated several beneficial properties as drug-carrier, limited drug-loading and expulsion of drug during storage led to the development of NLCs. However, the superiority of NLCs over SLNs has not been fully established yet due to the contradictory results. In this study, SLNs and NLCs were developed using clotrimazole as model drug. Size, polydispersity index (PI), zeta potential (ZP), drug-loading (L), drug encapsulation efficiency (EE), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD), drug release and stability of SLNs and NLCs were compared. Critical process parameters exhibited significant impact on the nanoparticles' properties. Size, PI, ZP and EE of the developed SLNs and NLCs were <100 nm, <0.17, <-22 mV and >82%, respectively. SEM images of SLNs and NLCs revealed spherical shaped particles (similar to 100 nm). DSC and XRD studies indicated slight difference between SLNs and NLCs as well as disappearance of the crystalline peak(s) of the encapsulated drug. NLCs demonstrated faster drug release than SLNs at low drug-loading, whereas there was no significant difference in drug release from SLNs and NLCs at high drug-loading. However, sustained/prolonged drug release was observed from both formulations. Furthermore, this study suggests that the drug release experiment should be designed considering the final application (topical/oral/parenteral) of the product. Regarding stability, NLCs showed better stability (in terms of size, PI, EE and L) than SLNs at 25 degrees C. Moreover, there was no significant difference in drug release profile of NLCs after 3 months storage in compare to fresh NLCs, while significant change in drug release rate was observed in case of SLNs. Therefore, NLCs have an edge over SLNs. (C) 2012 Elsevier B.V. All rights reserved.
引用
收藏
页码:139 / 151
页数:13
相关论文
共 35 条
[1]   Solid lipid nanoparticles as a drug delivery system for peptides and proteins [J].
Almeida, Antonio J. ;
Souto, Eliana .
ADVANCED DRUG DELIVERY REVIEWS, 2007, 59 (06) :478-490
[2]  
Brugnara C, 1995, Ann N Y Acad Sci, V763, P262, DOI 10.1111/j.1749-6632.1995.tb32411.x
[3]   Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: Physicochemical characterization and pharmacokinetics [J].
Chen, Chih-Chieh ;
Tsai, Tung-Hu ;
Huang, Zih-Rou ;
Fang, Jia-You .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2010, 74 (03) :474-482
[4]   DEVELOPMENT AND IN VITRO EVALUATIONS OF A LIPID NANOPARTICLE FORMULATTON CONTAINTNG TRETINOTN [J].
Das, Surajit ;
Wai Kiong Ng ;
Tan, Reginald B. H. .
NANOFORMULATION, 2012, 336 :38-52
[5]   Formulation design, preparation and physicochemical characterizations of solid lipid nanoparticles containing a hydrophobic drug: Effects of process variables [J].
Das, Surajit ;
Ng, Wai Kiong ;
Kanaujia, Parijat ;
Kim, Sanggu ;
Tan, Reginald B. H. .
COLLOIDS AND SURFACES B-BIOINTERFACES, 2011, 88 (01) :483-489
[6]   Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery [J].
Das, Surajit ;
Chaudhury, Anumita .
AAPS PHARMSCITECH, 2011, 12 (01) :62-76
[7]   Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN™) dispersions [J].
Freitas, C ;
Muller, RH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1998, 168 (02) :221-229
[8]   Correlation between long-term stability of solid lipid nanoparticles (SLN™) and crystallinity of the lipid phase [J].
Freitas, C ;
Müller, RH .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 1999, 47 (02) :125-132
[9]   Effect of a high-fat meal on absorption and disposition of lipophilic compounds: The importance of degree of association with triglyceride-rich lipoproteins [J].
Gershkovich, Pavel ;
Hoffman, Amnon .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2007, 32 (01) :24-32
[10]   Pharmacokinetic evaluation of oral fenofibrate nanosuspensions and SLN in comparison to conventional suspensions of micronized drug [J].
Hanafy, A. ;
Spahn-Langguth, H. ;
Vergnault, G. ;
Grenier, P. ;
Grozdanis, M. Tubic ;
Lenhardt, T. ;
Langguth, P. .
ADVANCED DRUG DELIVERY REVIEWS, 2007, 59 (06) :419-426