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Development and evaluation of a novel drug delivery: Soluplus®/TPGS mixed micelles loaded with piperine in vitro and in vivo.
Drug Dev Ind Pharm. 2018 Sep; 44(9):1409-1416.DD

Abstract

BACKGROUND

Although piperine can inhibit cells of tumors, the poor water solubility restricted its clinical application. This paper aimed to develop mixed micelles based on Soluplus® and D-α-tocopherol polyethylene glycol succinate (TPGS) to improve the aqueous solubility and anti-cancer effect.

METHODS

Piperine-loaded mixed micelles were prepared using a thin-film hydration method, and their physicochemical properties were characterized. The cellular uptake of the micelles was confirmed by confocal laser scanning microscopy in A549 lung cancer cells and HepG2 liver cancer cells. In addition, cytotoxicity of the piperine mixed micelles was studied in A549 lung cancer cells and HepG2 liver cancer cells. Free piperine or piperine-loaded Soluplus®/TPGS mixed micelles were administered at an equivalent dose of piperine at 3.2 mg/kg via a single intravenous injection in the tail vain for the pharmacokinetic study in vivo.

RESULTS

The diameter of piperine-loaded Soluplus®/TPGS (4:1) mixed micelles was about 61.9 nm and the zeta potential -1.16 ± 1.06 mV with 90.9% of drug encapsulation efficiency and 4.67% of drug-loading efficiency. Differential scanning calorimetry (DSC) studies confirmed that piperine is encapsulated by the Soluplus®/TPGS. The release results in vitro showed that the piperine-loaded Soluplus®/TPGS mixed micelles presented sustained release behavior compared to the free piperine. The mixed micelles exhibited better antitumor efficacy compared to free piperine and physical mixture against in A549 and HepG2 cells by MTT assay. The pharmacokinetic study revealed that the AUC of piperine-loaded mixed micelles was 2.56 times higher than that of piperine and the MRT for piperine-loaded mixed micelles was 1.2-fold higher than piperine (p < .05).

CONCLUSION

The results of the study suggested that the piperine-loaded mixed micelles developed might be a potential nano-drug delivery system for cancer chemotherapy. These results demonstrated that piperine-loaded Soluplus®/TPGS mixed micelles are an effective strategy to deliver piperine for cancer therapy.

Authors+Show Affiliations

a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.b College of Basic Medical Sciences , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.a School of Pharmacy , Dalian Medical University , Dalian , P.R. China.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29718714

Citation

Ding, Yingying, et al. "Development and Evaluation of a Novel Drug Delivery: Soluplus®/TPGS Mixed Micelles Loaded With Piperine in Vitro and in Vivo." Drug Development and Industrial Pharmacy, vol. 44, no. 9, 2018, pp. 1409-1416.
Ding Y, Wang C, Wang Y, et al. Development and evaluation of a novel drug delivery: Soluplus®/TPGS mixed micelles loaded with piperine in vitro and in vivo. Drug Dev Ind Pharm. 2018;44(9):1409-1416.
Ding, Y., Wang, C., Wang, Y., Xu, Y., Zhao, J., Gao, M., Ding, Y., Peng, J., & Li, L. (2018). Development and evaluation of a novel drug delivery: Soluplus®/TPGS mixed micelles loaded with piperine in vitro and in vivo. Drug Development and Industrial Pharmacy, 44(9), 1409-1416. https://doi.org/10.1080/03639045.2018.1472277
Ding Y, et al. Development and Evaluation of a Novel Drug Delivery: Soluplus®/TPGS Mixed Micelles Loaded With Piperine in Vitro and in Vivo. Drug Dev Ind Pharm. 2018;44(9):1409-1416. PubMed PMID: 29718714.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development and evaluation of a novel drug delivery: Soluplus®/TPGS mixed micelles loaded with piperine in vitro and in vivo. AU - Ding,Yingying, AU - Wang,Changyuan, AU - Wang,Yutong, AU - Xu,Youwei, AU - Zhao,Jing, AU - Gao,Meng, AU - Ding,Yanfang, AU - Peng,Jinyong, AU - Li,Lei, Y1 - 2018/05/27/ PY - 2018/5/3/pubmed PY - 2018/10/17/medline PY - 2018/5/3/entrez KW - Piperine KW - Soluplus® KW - TPGS KW - cancer therapy KW - mixed micelles SP - 1409 EP - 1416 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 9 N2 - BACKGROUND: Although piperine can inhibit cells of tumors, the poor water solubility restricted its clinical application. This paper aimed to develop mixed micelles based on Soluplus® and D-α-tocopherol polyethylene glycol succinate (TPGS) to improve the aqueous solubility and anti-cancer effect. METHODS: Piperine-loaded mixed micelles were prepared using a thin-film hydration method, and their physicochemical properties were characterized. The cellular uptake of the micelles was confirmed by confocal laser scanning microscopy in A549 lung cancer cells and HepG2 liver cancer cells. In addition, cytotoxicity of the piperine mixed micelles was studied in A549 lung cancer cells and HepG2 liver cancer cells. Free piperine or piperine-loaded Soluplus®/TPGS mixed micelles were administered at an equivalent dose of piperine at 3.2 mg/kg via a single intravenous injection in the tail vain for the pharmacokinetic study in vivo. RESULTS: The diameter of piperine-loaded Soluplus®/TPGS (4:1) mixed micelles was about 61.9 nm and the zeta potential -1.16 ± 1.06 mV with 90.9% of drug encapsulation efficiency and 4.67% of drug-loading efficiency. Differential scanning calorimetry (DSC) studies confirmed that piperine is encapsulated by the Soluplus®/TPGS. The release results in vitro showed that the piperine-loaded Soluplus®/TPGS mixed micelles presented sustained release behavior compared to the free piperine. The mixed micelles exhibited better antitumor efficacy compared to free piperine and physical mixture against in A549 and HepG2 cells by MTT assay. The pharmacokinetic study revealed that the AUC of piperine-loaded mixed micelles was 2.56 times higher than that of piperine and the MRT for piperine-loaded mixed micelles was 1.2-fold higher than piperine (p < .05). CONCLUSION: The results of the study suggested that the piperine-loaded mixed micelles developed might be a potential nano-drug delivery system for cancer chemotherapy. These results demonstrated that piperine-loaded Soluplus®/TPGS mixed micelles are an effective strategy to deliver piperine for cancer therapy. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/29718714/Development_and_evaluation_of_a_novel_drug_delivery:_Soluplus®/TPGS_mixed_micelles_loaded_with_piperine_in_vitro_and_in_vivo_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2018.1472277 DB - PRIME DP - Unbound Medicine ER -