Preparation and characterization of nano liposomes of Orthosiphon stamineus ethanolic extract in soybean phospholipids

BMC Biotechnology

Abdalrahim FA Aisha¹  Amin Malik Shah Abdul Majid³  Zhari Ismail² 

[1] Department of Pharmacy, School of Medicine and Health Sciences, An Najah National University, Nablus, West Bank, Palestine

[2] Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Universiti Sains Malaysia (USM), Minden 11800, Pulau Pinang, Malaysia

[3] Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia (USM), Minden 11800, Pulau Pinang, Malaysia

关键词: Liposomal drug delivery system;    Soybean phospholipids;    Soybean lecithin;    Orthosiphon stamineus;   

Others  :  834884
DOI  :  10.1186/1472-6750-14-23

 received in 2013-03-03, accepted in 2014-03-17,  发布年份 2014

【 摘 要 】

Background

O. stamineus is a medicinal herb with remarkable pharmacological properties. However, poor solubility of the active principles limits its medicinal value. This study sought to prepare nano liposomes of OS ethanolic extract in unpurified soybean phospholipids in order to improve its solubility and permeability. OS liposomes were prepared by the conventional film method, and were characterized for solubility, entrapment efficiency, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), particle size and zeta potential, release, absorption in everted rat intestinal sacs, and DPPH scavenging effect.

Results

OS liposomes showed substantial enhancement of extract’s solubility from 956 ± 34 to 3979 ± 139 μg/ml, with entrapment efficiency of 66.2 ± 0.9%. FTIR study indicates interaction between soybean phospholipids and OS extract. TEM and dynamic light scattering showed presence of round anionic nano liposomes with particle size and zeta potential of 152.5 ± 1.1 nm and −49.8 ± 1.0 mV, respectively. A study using the fluorescent probe pyrene showed the critical micellar concentration is 9.2 ± 2.9 μg/ml. Release studies showed 94 ± 0.1% release in non-formulated extract and 62.4 ± 0.1% in OS liposomes. Released extract from OS liposomes showed improvement in DPPH scavenging effect, IC50 = 23.5 ± 1.1 μg/ml compared to 32.4 ± 0.5 μg/ml in non-formulated extract. OS liposomes were stable at pH 5.5 and 7.4, but showed reversible agglomeration at pH 1.6. Absorption in everted rat intestinal sacs showed substantial improvement in permeability of 3′-hydroxy-5, 6, 7, 4″-tetramethoxyflavone, sinensetin, eupatorin, and 3 other unknown compounds.

Conclusions

Enhanced solubility, absorption and antioxidant effect may improve the overall pharmacological effects and medicinal value of OS ethanolic extract.

【 授权许可】

   
2014 Aisha et al.; licensee BioMed Central Ltd.

【 图 表 】

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