mPEG-PLA Micelle for Delivery of Effective Parts of Andrographis Paniculata

Title:mPEG-PLA Micelle for Delivery of Effective Parts of Andrographis Paniculata

Volume: 15 Issue: 4

Author(s): Hailu Yao, Shiyong Song, Xiaolu Miao, Xiao Liu, Junli Zhao, Zhen Wang, Xiaoting Shao, Yu Zhang*Guang Han*

Affiliation:

• Institute of Pharmacy, Pharmacy College of Henan University, Kaifeng,China

• Institute of Pharmacy, Pharmacy College of Henan University, Kaifeng,China

Keywords: Andrographis paniculata, cell cytotoxicity, drug entrapping efficiency, drug loading capacity, micelle, size, solubility, stability.

Abstract: Background: Many studies have shown that Andrographis paniculata (Burm. f.) Nees has a good anti-tumor effect, but poor solubility in water and poor bioavailability hinder the modernization of it.

Method: To formulate the effective parts (mainly diterpene lactones) of Andrographis paniculata (AEP) into targeting drug delivery system, a series of poly(ethylene glycol)-poly(D.L-lactic acid)(mPEG-PLA) with different ratio of hydrophilic and hydrophobic segment was synthetized to encapsulate AEP. AEP micelles were prepared by a simple solvent-evaporation method. According to the loading capacity, the best polymer was chosen. mPEG-PLA micelles were characterized in terms of drug entrapping efficiency, loading capacity, size, the crystalline state of AEP, stability and release profile. Meanwhile, the cytotoxicity of micelles on mouse breast cancer 4T-1 was investigated.

Results: These micelle (mPEG-PLA-AEP) particles had a size of (92.84±5.63) nm and a high entrapping efficiency and loading capacity of (91.00±11.53)% and (32.14±3.02)%(w/w), respectively. The powder DSC showed that drugs were well encapsulated in the core of micelles. mPEG-PLA-AEP had a good stability against salt dissociation, protein adsorption and anion substitution and the solubility of andrographolide (AG) and 14-deoxy-11,12-didehydroandrographolide(DDAG) in AEP increased 4.51 times and 2.12 times in water, and the solubility of DAG showed no difference. mPEG-PLA-AEP had the same release profile in different dissolution medium. Cytotoxicity testing in vitro demonstrated that mPEG-PLA-AEP exhibited higher cell viability inhibition in mouse breast cancer 4T-1 than free AEP.

Conclusion: mPEG-PLA micelles offer a promising alternative for TCM therapy with higher solubility and improved antitumor effect.

Cite this article as:

Yao Hailu , Song Shiyong , Miao Xiaolu, Liu Xiao, Zhao Junli , Wang Zhen , Shao Xiaoting , Zhang Yu*, Han Guang*, mPEG-PLA Micelle for Delivery of Effective Parts of Andrographis Paniculata, Current Drug Delivery 2018; 15 (4) . https://dx.doi.org/10.2174/1567201814666171120113521