Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 47, Issue 1, Pages 139-151Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2012.05.010
Keywords
Solid lipid nanoparticle; Nanostructured lipid carrier; Clotrimazole; Characterization; Drug release; Stability
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Funding
- Science and Engineering Research Council of A*STAR (Agency for Science, Technology and Research), Singapore [ICES/10-125A01]
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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.
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