当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF PHARMACEUTICS期刊下所有文献 > Preparation of an injectable depot system for long-term delivery of alendronate and evaluation of its anti-osteoporotic effect in an ovariectomized rat model.

Preparation of an injectable depot system for long-term delivery of alendronate and evaluation of its anti-osteoporotic effect in an ovariectomized rat model.

Abstract：

:We prepared an injectable depot system for the long-term delivery of alendronate using a solid/water/oil/water multiple emulsion technique with poly(lactic-co-glycolic acid) as a carrier. The microparticles were spherical with smooth surfaces, ranging from 20 to 70 μm in size. The microspheres (ALD-HA-RG504H-MC70) were optimally prepared by introducing a viscous material (hyaluronic acid) and a co-solvent system in the inner aqueous and oil phases, respectively, and showed a significantly increased drug encapsulation efficacy (>70%); the initial burst release was <10% after 1 day. In vitro drug release from ALD-HA-RG504H-MC70 followed zero-order kinetics for approximately 4 weeks and the alendronate plasma level was maintained for more than 1 month after intramuscular injection in rabbits. The ovariectomized (OVX) rats with ALD-HA-RG504H-MC70 injected intramuscularly (0.9 mg alendronate/kg/4 weeks) had 112% and 482% increased bone mineral density and trabecular area in the tibia than the OVX controls, respectively, and showed significant improvements in trabecular microarchitecture and bone strength. Furthermore, the major biomarkers of bone turnover revealed that ALD-HA-RG504H-MC70 suppressed effectively the progression of osteoporosis and facilitated new bone formation. Therefore, this sustained release depot system may improve patient compliance and therapeutic efficacy by reducing dose amounts and frequency with minimal adverse reactions.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Bae J,Park JW

doi

10.1016/j.ijpharm.2015.01.020

subject

Has Abstract

pub_date

2015-03-01 00:00:00

pages

37-47

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(15)00022-8

journal_volume

480

pub_type

杂志文章

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