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Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation.
Pharm Biol. 2016; 54(1):130-8.PB

Abstract

CONTEXT

Capsaicin (CAP) is an effective drug in the treatment of pain and cancer. However, its practical administration has been limited due to poor aqueous solubility and bioavailability, as well as strong gastrointestinal irritation.

OBJECTIVE

The objective of this study is to improve the solubility and oral bioavailability of CAP by reducing irritation via hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex formulation, in vitro and in vivo analysis.

MATERIALS AND METHODS

The complex (CAP-HP-β-CD) was developed via the magnetic stirring method and characterized using ultraviolet (UV) absorption spectrometry, infrared radiation (IR) spectroscopy, and differential scanning calorimetry (DSC). Rats were treated with CAP (90 mg × kg(-1)) or CAP-HP-β-CD (corresponding to 90 mg × kg(-1) CAP) by gavage, and all the plasma samples were analyzed with high performance liquid chromatography (HPLC).

RESULTS

The results of UV, IR, and DSC showed that an acceptable CAP-HP-β-CD (encapsulation efficiency, 75.83%; drug loading, 7.44%) was formulated. In vitro release study of CAP-HP-β-CD revealed that the cumulative release of CAP from HP-β-CD encapsulation was obviously enhanced (above 80% increases). Similarly, the in vivo pharmacokinetics parameters also increased, Cmax (from 737.94 to 1117.57 ng × mL(-1)), AUC0- (from 5285.9 to 7409.8 ng × h × mL(-1)) or relative bioavailability (139.38%). The gastric irritation bioassay further showed that the CAP-HP-β-CD was far better than free CAP.

DISCUSSION AND CONCLUSION

CAP exhibited significant aqueous solubility and oral bioavailability, as well as minimal irritation effect after forming inclusion complex with HP-β-CD. Therefore, these findings could provide an equally important alternative option for the clinical use of CAP.

Authors+Show Affiliations

a Department of Pharmaceutics , School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang , China and.a Department of Pharmaceutics , School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang , China and.a Department of Pharmaceutics , School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang , China and.a Department of Pharmaceutics , School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang , China and.a Department of Pharmaceutics , School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang , China and.a Department of Pharmaceutics , School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University , Zhenjiang , China and.b Nanjing Institute for Comprehensive Utilization of Wild Plants , Nanjing , China.

Pub Type(s)

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

Language

eng

PubMed ID

25853954

Citation

Zhao, Yingying, et al. "Preparation, Characterization, and Pharmacokinetics Study of Capsaicin Via Hydroxypropyl-beta-cyclodextrin Encapsulation." Pharmaceutical Biology, vol. 54, no. 1, 2016, pp. 130-8.
Zhao Y, Sun C, Shi F, et al. Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation. Pharm Biol. 2016;54(1):130-8.
Zhao, Y., Sun, C., Shi, F., Firempong, C. K., Yu, J., Xu, X., & Zhang, W. (2016). Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation. Pharmaceutical Biology, 54(1), 130-8. https://doi.org/10.3109/13880209.2015.1021816
Zhao Y, et al. Preparation, Characterization, and Pharmacokinetics Study of Capsaicin Via Hydroxypropyl-beta-cyclodextrin Encapsulation. Pharm Biol. 2016;54(1):130-8. PubMed PMID: 25853954.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation, characterization, and pharmacokinetics study of capsaicin via hydroxypropyl-beta-cyclodextrin encapsulation. AU - Zhao,Yingying, AU - Sun,Chaonan, AU - Shi,Feng, AU - Firempong,Caleb Kesse, AU - Yu,Jiangnan, AU - Xu,Ximing, AU - Zhang,Weiming, Y1 - 2015/04/08/ PY - 2015/4/9/entrez PY - 2015/4/9/pubmed PY - 2016/9/22/medline KW - HP-β-CD KW - in vitro release KW - irritation KW - oral bioavailability SP - 130 EP - 8 JF - Pharmaceutical biology JO - Pharm Biol VL - 54 IS - 1 N2 - CONTEXT: Capsaicin (CAP) is an effective drug in the treatment of pain and cancer. However, its practical administration has been limited due to poor aqueous solubility and bioavailability, as well as strong gastrointestinal irritation. OBJECTIVE: The objective of this study is to improve the solubility and oral bioavailability of CAP by reducing irritation via hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex formulation, in vitro and in vivo analysis. MATERIALS AND METHODS: The complex (CAP-HP-β-CD) was developed via the magnetic stirring method and characterized using ultraviolet (UV) absorption spectrometry, infrared radiation (IR) spectroscopy, and differential scanning calorimetry (DSC). Rats were treated with CAP (90 mg × kg(-1)) or CAP-HP-β-CD (corresponding to 90 mg × kg(-1) CAP) by gavage, and all the plasma samples were analyzed with high performance liquid chromatography (HPLC). RESULTS: The results of UV, IR, and DSC showed that an acceptable CAP-HP-β-CD (encapsulation efficiency, 75.83%; drug loading, 7.44%) was formulated. In vitro release study of CAP-HP-β-CD revealed that the cumulative release of CAP from HP-β-CD encapsulation was obviously enhanced (above 80% increases). Similarly, the in vivo pharmacokinetics parameters also increased, Cmax (from 737.94 to 1117.57 ng × mL(-1)), AUC0- (from 5285.9 to 7409.8 ng × h × mL(-1)) or relative bioavailability (139.38%). The gastric irritation bioassay further showed that the CAP-HP-β-CD was far better than free CAP. DISCUSSION AND CONCLUSION: CAP exhibited significant aqueous solubility and oral bioavailability, as well as minimal irritation effect after forming inclusion complex with HP-β-CD. Therefore, these findings could provide an equally important alternative option for the clinical use of CAP. SN - 1744-5116 UR - https://www.unboundmedicine.com/medline/citation/25853954/Preparation_characterization_and_pharmacokinetics_study_of_capsaicin_via_hydroxypropyl_beta_cyclodextrin_encapsulation_ L2 - https://www.tandfonline.com/doi/full/10.3109/13880209.2015.1021816 DB - PRIME DP - Unbound Medicine ER -