Development and evaluation of penciclovir-loaded solid lipid nanoparticles for topical delivery

被引:174
作者
Lv, Qingzhi [1 ]
Yu, Aihua [1 ]
Xi, Yanwei [1 ]
Li, Houli [1 ]
Song, Zhimei [1 ,2 ]
Cui, Jing [3 ]
Cao, Fengliang [1 ]
Zhai, Guangxi [1 ]
机构
[1] Shandong Univ, Dept Pharmaceut, Coll Pharm, Jinan 250012, Peoples R China
[2] Jinan Univ, Dept Chem & Pharmaceut, Coll Chem, Jinan 250022, Peoples R China
[3] Shandong Univ, Dept Pharm, Qilu Hosp, Jinan 250012, Peoples R China
关键词
Penciclovir; HSV; Solid lipid nanoparticles; DSC; Skin targeting; Skin permeation; IN-VITRO RELEASE; DRUG CARRIERS; SKIN; SLN; MICROEMULSION; FORMULATION; ACYCLOVIR; NLC;
D O I
10.1016/j.ijpharm.2009.01.014
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The objective of this investigation was to develop solid lipid nanoparticles (SLNs) of penciclovir and evaluate the potential of SLNs as the carrier of penciclovir for topical delivery. Penciclovir-loaded SLNs were prepared by a double (W/O/W) emulsion technique. The SLNs presented spherical with the mean diameter of 254.9 nm. The entrapment efficiency, drug loading and zeta potential were 92.40%,4.62% and -25.0 mV, respectively. DSC study showed that penciclovir encapsulated in SLNs was in the amorphous form. The cumulative amount of penciclovir penetrated through excised rat skin from SLNs was more than 2-fold that of the commercial cream as a control at 12 h after administration. There was no significant difference of penciclovir content deposited in epidermis between the cream and SLNs administrated for 2, 6 and 12 h, while SLNs increased the cumulative uptake of penciclovir in dermis significantly at the same intervals. Microscopic pictures showed that the interaction between SLNs and the skin surface changed the apparent morphology of stratum corneum, and broke the close conjugation of corneocyte layers, which was the possible reason that SLNs increased the permeation of penciclovir into skin dermis. It can be concluded from our study that SLNs provide a good skin targeting effect and may be a promising carrier for topical delivery of penciclovir. (c) 2009 Elsevier B.V. All rights reserved.
引用
收藏
页码:191 / 198
页数:8
相关论文
共 50 条
[1]   Penciclovir solubility in Eudragit films: a comparison of X-ray, thermal, microscopic and release rate techniques [J].
Ahmed, A ;
Barry, BW ;
Williams, AC ;
Davis, AF .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2004, 34 (05) :945-956
[2]   In vitro selection of drug-resistant varicella-zoster virus (VZV) mutants (OKA strain): differences between acyclovir and penciclovir? [J].
Andrei, G ;
De Clercq, E ;
Snoeck, R .
ANTIVIRAL RESEARCH, 2004, 61 (03) :181-187
[3]  
Andya JD, 2003, AAPS PHARMSCI, V5
[4]   Microemulsions for topical delivery of 8-methoxsalen [J].
Baroli, B ;
López-Quintela, MA ;
Delgado-Charro, MB ;
Fadda, AM ;
Blanco-Méndez, J .
JOURNAL OF CONTROLLED RELEASE, 2000, 69 (01) :209-218
[5]  
BOUWSTRA JA, 1995, J LIPID RES, V36, P685
[6]   Lipid vesicles and other colloids as drug carriers on the skin [J].
Cevc, G .
ADVANCED DRUG DELIVERY REVIEWS, 2004, 56 (05) :675-711
[7]   Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting [J].
Chen, HB ;
Chang, XL ;
Du, DR ;
Liu, W ;
Liu, J ;
Weng, T ;
Yang, YJ ;
Xu, HB ;
Yang, XL .
JOURNAL OF CONTROLLED RELEASE, 2006, 110 (02) :296-306
[8]   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
[9]   Development and validation of a high-performance liquid chromatographic method for the determination of cyproterone acetate in human skin [J].
de Hassonville, SH ;
Chiap, P ;
Liégeois, JF ;
Evrard, B ;
Delattre, L ;
Crommen, J ;
Piel, G ;
Hubert, P .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2004, 36 (01) :133-143
[10]   Liposomes and skin: From drug delivery to model membranes [J].
El Maghraby, G. M. ;
Barry, B. W. ;
Williams, A. C. .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 34 (4-5) :203-222