Design of a transdermal formulation containing raloxifene nanoparticles for osteoporosis treatment

• DOI: 10.2147/ijn.s173216
• Publication Date: 2018-09-06T02:26:37Z
• Authors: Noriaki Nagai; Fumihiko Ogata; Hiroko Otake; Yosuke Nakazawa; Naohito Kawasaki
• Keywords: Raloxifene; Penetration (warfare)

In the clinical setting, raloxifene, a second-generation selective estrogen receptor modulator, is administered orally; however, bioavailability (BA) only 2% because of its poor solubility in aqueous fluids and extensive first-pass metabolism. Therefore, it expected that development transdermally delivered formulation may reduce necessary dose without compromising therapeutic efficacy. this study, we designed transdermal formulations containing raloxifene nanoparticles evaluated their usefulness for osteoporosis therapy.Raloxifene was crushed with methylcellulose by bead mill method, milled gelled or menthol (a permeation enhancer) Carbopol® 934 (without menthol, Ral-NPs; mRal-NPs). The drug release penetration were measured using Franz diffusion cell, evaluation determined an ovariectomized rat model.The mean particle size (Ral-NPs) 173.7 nm. Although released from Ral-NPs remained nanoparticle state, skin prevented stratum corneum rat. On other hand, inclusion attenuated barrier function permitted through skin. Moreover, macropinocytosis relates to including (mRal-NPs), since inhibited treatment 2 µM rottlerin, inhibitor. addition, application 0.3% mRal-NPs (once day) decreases calcium level stiffness bones rat.We prepared solid method novel enhancers. These trans-dermal overcome properties show high route (BA 8.5%). found are useful