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Emodin loaded solid lipid nanoparticles: preparation, characterization and antitumor activity studies.
Int J Pharm 2012; 430(1-2):238-46IJ

Abstract

The objective of the present study was to prepare and characterize emodin (EMO)-loaded solid lipid nanoparticles (E-SLNs) and evaluate their antitumor activity in vitro. EMO and pharmaceutical lipid material were used to prepare E-SLNs by high pressure homogenization (HPH). Poloxamer 188 and Tween 80 were used as surfactants. The physicochemical properties of the E-SLNs were investigated by particle size analysis, zeta potential measurement, drug entrapment efficiency (EE), stability and in vitro drug release behavior. The E-SLNs showed stable particle size at 28.6 ± 3.1 nm, ideal drug EE and relative long-term physical stability after being stored for 4 months. The drug release of E-SLNs could last 72 h and exhibited a sustained profile, which made it a promising vehicle for oral drug delivery. MTT assay showed that E-SLNs could significantly enhance the in vitro cytotoxicity against human breast cancer cell line MCF-7 and MDA-MB-231 cells compared to the EMO solution, while free EMO, blank SLNs (B-SLNs) and E-SLNs all showed no significant toxicity to human mammary epithelial line MCF-10A cells. Flow cytometric analysis demonstrated that E-SLNs also showed more significant cell cycle arrest effect in MCF-7 cells compared to bulk EMO solution. Hoechst 33342 staining and Annexin V-FITC/PI double staining further confirmed that E-SLNs induced higher apoptotic rates in MCF-7 cells, indicating that cell cycle arrest and apoptosis maybe the underlying mechanism of the enhanced cytotoxicity. Taken together, it seems that HPH was a simple, available and effective method for preparing high quality E-SLNs to enhance its aqueous solubility. Moreover, these results suggest that the delivery of EMO as lipid nanoparticles maybe a promising approach for cancer therapy.

Authors+Show Affiliations

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Av. Padre Tomas Pereira S.J., Taipa, Macau, 999078, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22465546

Citation

Wang, Shengpeng, et al. "Emodin Loaded Solid Lipid Nanoparticles: Preparation, Characterization and Antitumor Activity Studies." International Journal of Pharmaceutics, vol. 430, no. 1-2, 2012, pp. 238-46.
Wang S, Chen T, Chen R, et al. Emodin loaded solid lipid nanoparticles: preparation, characterization and antitumor activity studies. Int J Pharm. 2012;430(1-2):238-46.
Wang, S., Chen, T., Chen, R., Hu, Y., Chen, M., & Wang, Y. (2012). Emodin loaded solid lipid nanoparticles: preparation, characterization and antitumor activity studies. International Journal of Pharmaceutics, 430(1-2), pp. 238-46. doi:10.1016/j.ijpharm.2012.03.027.
Wang S, et al. Emodin Loaded Solid Lipid Nanoparticles: Preparation, Characterization and Antitumor Activity Studies. Int J Pharm. 2012 Jul 1;430(1-2):238-46. PubMed PMID: 22465546.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Emodin loaded solid lipid nanoparticles: preparation, characterization and antitumor activity studies. AU - Wang,Shengpeng, AU - Chen,Tongkai, AU - Chen,Ruie, AU - Hu,Yangyang, AU - Chen,Meiwan, AU - Wang,Yitao, Y1 - 2012/03/23/ PY - 2011/11/22/received PY - 2012/02/24/revised PY - 2012/03/16/accepted PY - 2012/4/3/entrez PY - 2012/4/3/pubmed PY - 2012/9/29/medline SP - 238 EP - 46 JF - International journal of pharmaceutics JO - Int J Pharm VL - 430 IS - 1-2 N2 - The objective of the present study was to prepare and characterize emodin (EMO)-loaded solid lipid nanoparticles (E-SLNs) and evaluate their antitumor activity in vitro. EMO and pharmaceutical lipid material were used to prepare E-SLNs by high pressure homogenization (HPH). Poloxamer 188 and Tween 80 were used as surfactants. The physicochemical properties of the E-SLNs were investigated by particle size analysis, zeta potential measurement, drug entrapment efficiency (EE), stability and in vitro drug release behavior. The E-SLNs showed stable particle size at 28.6 ± 3.1 nm, ideal drug EE and relative long-term physical stability after being stored for 4 months. The drug release of E-SLNs could last 72 h and exhibited a sustained profile, which made it a promising vehicle for oral drug delivery. MTT assay showed that E-SLNs could significantly enhance the in vitro cytotoxicity against human breast cancer cell line MCF-7 and MDA-MB-231 cells compared to the EMO solution, while free EMO, blank SLNs (B-SLNs) and E-SLNs all showed no significant toxicity to human mammary epithelial line MCF-10A cells. Flow cytometric analysis demonstrated that E-SLNs also showed more significant cell cycle arrest effect in MCF-7 cells compared to bulk EMO solution. Hoechst 33342 staining and Annexin V-FITC/PI double staining further confirmed that E-SLNs induced higher apoptotic rates in MCF-7 cells, indicating that cell cycle arrest and apoptosis maybe the underlying mechanism of the enhanced cytotoxicity. Taken together, it seems that HPH was a simple, available and effective method for preparing high quality E-SLNs to enhance its aqueous solubility. Moreover, these results suggest that the delivery of EMO as lipid nanoparticles maybe a promising approach for cancer therapy. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/22465546/Emodin_loaded_solid_lipid_nanoparticles:_preparation_characterization_and_antitumor_activity_studies_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(12)00268-2 DB - PRIME DP - Unbound Medicine ER -