A Novel Solid-in-oil Nanosuspension for Transdermal Delivery of Diclofenac Sodium
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We formulated a solid-in-oil nanosuspension (SONS) as a novel transdermal delivery carrier for diclofenac sodium (DFNa). The basic transdermal characteristics of the SONS were evaluated using a Yucatan micropig (YMP) skin model.
DFNa-sucrose erucate (i.e. surfactant) complexes were prepared via the formation of a water-in-oil emulsion. The complexes were suspended in isopropyl myristate (IPM) to form a SONS. The basic transdermal characteristics of the SONS were examined using full-thickness YMP dorsal skin in a Franz-type diffusion cell. DFNa powder suspended in IPM without complex formation was used as a control. The effect of the weight ratio of surfactant to DFNa on DFNa penetration of the skin was evaluated.
DFNa was successfully dispersed into IPM as a nanosized suspension via complex formation with sucrose erucate. The resultant SONS increased the permeability flux of DFNa across the YMP skin by up to 3.8-fold compared with the control. The size of the SONS depended on the weight ratio of the surfactant to DFNa. The optimal weight ratio for the highest DFNa permeation was 8.8, at which point the mean diameter of the SONS was 14.4 nm.
The SONS formulation can enhance the percutaneous absorption of DFNa.
- E. C. Ku, J. M. Wasvary, and W. D. Cash. Diclofenac sodium (GP 45840, Voltaren), a potent inhibitor of prostaglandin synthetase. Biochem. Pharmacol. 24:641–643 (1975). CrossRef
- C. Sakamoto. NSAIDs caused gastric mucosal injury: with a special reference to COX-2. J. Nippon Med. Sch. 70:5–11 (2003). CrossRef
- R. Grahame. Transdermal non-steroidal anti-inflammatory agents. Br. J. Clin. Pract. 49:33–35 (1995).
- G. L. Flynn and B. Stewart. Percutaneous drug penetration: choosing candidates for transdermal development. Drug Dev. Res. 13:169–185 (1988). CrossRef
- M. Müller, H. Mascher, C. Kikuta, S. schäfer, M. Brunner, G. Dorner, and H. G. Eichler. Diclofenac concentrations in defined tissue layers after topical administration. Clin. Pharmacol. Ther. 62:292–299 (1997).
- A. Arellano, S. Santoyo, C. Martin, and P. Ygartua. Enhancing of terpenes on the in vitro percutaneous absorption of diclofenac sodium. Int. J. Pharm. 130:141–145 (1996). CrossRef
- A. Arellano, S. Santoyo, C. Martin, and P. Ygartua. Influence of propylene glycol and isopropyl myristate on the in vitro percutaneous penetration of diclofenac sodium from carbopol gels. Eur. J. Pharm. Sci. 7:129–135 (1998). CrossRef
- S. Naito and H. Tominaga. Percutaneous absorption of diclofenac sodium ointment. Int. J. Pharm. 24:115–124 (1985). CrossRef
- R. R. Boinpally, S. L. Zhou, S. Poondru, G. Devraj, and B. R. Jasti. Lecithin vesicles for topical delivery of diclofenac. Eur. J. Pharm. Biopharm. 56:389–392 (2003). CrossRef
- E. Escribano, A. C. Calpena, J. Queralt, R. Obach, and J. Domenech. Assessment of diclofenac permeation with different formulations: anti-inflammatory study of a selected formula. Eur. J. Pharm. Sci. 19:203–210 (2003). CrossRef
- F. Dreher, P. Walde, P. Walther, and E. Wehrli. Interaction of a lecithin microemulsion gel with human Stratum corneum and its effect on transdermal transport. J. Control. Release. 45:131–140 (1997). CrossRef
- K. Takahashi, H. Sakano, N. Numata, S. Kuroda, and N. Mizuno. Effect of fatty acid diesters on permeation of Anti-inflammatory drugs through rat skin. Drug Dev. Ind. Pharm. 10:1285–1294 (2002). CrossRef
- H. Piao, N. Kamiya, J. Watanabe, H. Yokoyama, A. Hirata, T. Fuijii, I. Shimizu, S. Ito, and M. Goto. Oral delivery of diclofenac sodium using a novel solid-in-oil suspension. Int. J. Pharm. 313:159–162 (2006). CrossRef
- C. S. Leopold and B. C. Lippold. An attempt of the penetration enhancing effects of lipophilic vesicles with differential scanning calorimetry (DSC). J. Pharm. Pharmacol. 47:276–281 (1995).
- P. Karande, A. Jain, K. Ergun, V. Kispersky, and S. Mitragotri. Design Principles of chemical penetration enhancers for transdermal drug delivery. Proc. Natl. Acad. Sci. USA 102:4688–4693 (2005). CrossRef
- M. E. Roberts and K. R. Mueller. Comparisons of in vitro nitroglycerin (TNG) flux across Yucatan pig, Hairless mouse, and Human skins. Pharm. Res. 7:673–676 (1990). CrossRef
- L. B. Lopes, J. H. Collett, M. Vitoria, and L. B. Bently. Topical delivery of cyclosporin A: an in vitro study using monoolein as a penetration enhancer. Eur. J. Pharm. Biopharm. 60:25–30 (2005). CrossRef
- A Novel Solid-in-oil Nanosuspension for Transdermal Delivery of Diclofenac Sodium
Volume 25, Issue 4 , pp 896-901
- Cover Date
- Print ISSN
- Online ISSN
- Springer US
- Additional Links
- diclofenac sodium
- isopropyl myristate
- solid-in-oil nanosuspension.
- sucrose ester
- transdermal delivery
- Yucatan micropig skin
- Industry Sectors
- Author Affiliations
- 1. Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, Fukuoka, 819-0395, Japan
- 2. Center for Future Chemistry, Kyushu University, Fukuoka, 819-0395, Japan
- 3. ASPION Corporation, Tokushima, Japan