Title:Synthesis and Evaluation of Bone Targeting PLGA Nanoparticles Loaded
with Components of Traditional Chinese Medicine Formulas
Volume: 18
Issue: 1
Author(s): Zehao Zhao, Yanling Deng, Yu Deng, Zhuojun Chen and Zhikun Zhou*
Affiliation:
- Department of Pharmacy, Guangdong Medical University, Dongguan, 523808, China
Keywords:
Poly(lactic-co-glycolic acid), nanoparticles, traditional Chinese medicine formula, bone targeting, osteoblasts, solvent evaporation.
Abstract:
Background: Targeted nanoparticles’ preparation can enhance local drug concentration and
reduce the side effects of drugs in non-targeted organs. At present, many patents have been applied for
in the field of bone-targeted nanoparticles’ preparations. They play an important role in the treatment
and diagnosis of diseases. In this experiment, nanoparticles with bone targeting function were prepared
by poly(lactic-co-glycolic acid) (PLGA) copolymer and tetracycline. These nanoparticles contain active
ingredients in the Huangqi Sanxian decoction, a kind of Traditional Chinese Medicine (TCM) compound
formula. These nanoparticles are predicted to be useful in the treatment of osteoporosis.
Methods: Synthesis of tetracycline targeting groups was performed by acylation reaction, and PLGA
nanoparticles were prepared by the Emulsification-solvent Evaporation Method. The appearance and
particle size of the product were evaluated, and the effects of nanoparticles on the physiological activities
of osteoblasts were observed. Finally, the bone-targeting ability of targeted nanoparticles in vivo
and in vitro was investigated.
Results: The average particle size of the nanoparticles was about 200 nm, and the average drug entrapment
was 60%. In vitro evaluation of osteoblasts assay showed that the nanoparticles can be well taken
by cells. Their good biocompatibility and sustained-release properties reduce the toxic side effects of
drugs when they promote osteoblasts’ physiological activities. The results of the in vitro and in vivo
bone targeting ability assays showed that tetracycline modified nanoparticles could effectively accumulate
in the bone, indicating the great bone-targeting ability of the nanoparticles. The use of PLGA to
load active components in the TCM compound formulas and remodel targeting groups is expected to
improve drug efficacy, reduce drug dosage, and effects on non- action sites. This may provide new ideas
for the development of TCM compound dosage forms.
Conclusion: In summary, we prepared PLGA nanoparticles of multiple TCM ingredients with bone targeting
ability, and they had good morphological appearance, and a promoting effect on various physiological
activities of osteoblasts.
