Bone-targeted delivery of simvastatin-loaded PEG-PLGA micelles conjugated with tetracycline for osteoporosis treatment

Drug Delivery and Translational Research
Yonghui XieXueying Tan

Abstract

This study aimed to investigate the improved therapeutic efficacy and pharmacokinetic profiles of simvastatin (SIM) with imparted bone targeting potential using tetracycline-mediated PEG-PLGA (TC-PEG-PLGA) micelles in osteoporotic rats. The SIM-loaded TC-PEG-PLGA (TC-PEG-PLGA/SIM) micelles were evaluated for particle size, morphology, stability, loading efficiency, cell viability, bone mineral binding ability in vitro, mineralization, pharmacokinetics, and pharmacodynamics. TC-PEG-PLGA conjugates were successfully and could self-assembly form micelles in aqueous medium with a 19.4 μg/mL critical micelle concentration. Then, TC-PEG-PLGA/SIM micelles were prepared with solvent diffusion method, and the obtained micelles (56.21 ± 7.39 nm average size; 81.8 ± 3.1% encapsulation efficiency; and 7.56 ± 0.27% drug loading) led to the prolonged release of SIM from micelles. Cellular uptake test indicated that TC had no effects on micellar internalization and micellar internalization was mainly involved with clathrin-mediated endocytic pathway. In vivo pharmacokinetic results indicated that TC-PEG-PLGA/SIM micelles exhibited a significantly prolonged time in systemic circulation and were preferentially accumulated in bone tissue. TC-PEG...Continue Reading

References

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Citations

Feb 18, 2020·Expert Opinion on Drug Delivery·David Medina-CruzThomas J Webster
Jul 7, 2020·Biochemical Society Transactions·Zi ZouCijun Shuai
Jan 17, 2020·Materials·Levi Collin Nelemans, Leonid Gurevich
Aug 21, 2020·Head & Face Medicine·Martin Mariano Isabelo SabandalSonja Sielker
Nov 19, 2021·Journal of Nanobiotechnology·Jingbo HuJin Liu

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Methods Mentioned

BETA
dynamic light scattering
transmission electron microscopy
X-ray
light microscopy
flow cytometry

Software Mentioned

Drug and Statistics Software ( DAS

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