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AAPS PharmSciTech

, 20:284 | Cite as

Self-Micro-Emulsifying Controlled Release of Eugenol Pellets: Preparation, In vitro/In vivo Investigation in Beagle Dogs

  • Qilong Wang
  • Min Guo
  • Michael Adu-Frimpong
  • Kangyi Zhang
  • Qiuxuan Yang
  • Elmurat Toreniyazov
  • Hao Ji
  • Ximing XuEmail author
  • Xia CaoEmail author
  • Jiangnan YuEmail author
Research Article
  • 11 Downloads

Abstract

This report aimed to formulate self-micro-emulsifying (SMEDDS) controlled-release pellets delivery system to improve aqueous solubility and in vivo availability of eugenol, a main constituent of clove oil with multiple pharmacological activities. The optimal formulation of eugenol-SMEDDS was eugenol: ethyl oleate: cremophor EL: 1, 2-propylene glycol at the ratio of 5:5:12:8. The SMEDDS were observed under transmission electron microscopy (TEM), and the size distribution was measured with dynamic laser light scatting (DLS). The particle size, index of dispersity (PDI), and zeta potential (Z-potential) were 68.8 ± 0.1 nm, 0.285 ± 0.031, and − 11.62 ± 0.63 mV, respectively. Eugenol-SMEDDS exhibited substantial increased in vitro dissolution compared with the free eugenol. The eugenol-SMEDDS sustained-release pellets (eugenol-SMEDDS-SR pellets) comprising of eugenol-SMEDDS, hydroxypropyl methylcellulose (HPMC), microcrystalline cellulose (MCC), and ethyl cellulose (EC) coats were obtained via extrusion spheronization technique. Consequently, the obtained pellets observed under scanning electron microscopy (SEM) showed spherical shape with smooth surface, desirable drug loading capacity (7.18 ± 0.17%), greater stability, and controlled release. Meanwhile, the oral test showed that bioavailability of eugenol in pellets was highly improved 23.6-fold to the free eugenol. Overall, these results suggested that the improvement of the oral bioavailability of eugenol-SMEDDS-SR could be due to the successful incorporation of the drug into SMEDDS.

KEY WORDS

eugenol SMEDDS sustained-release pellet drug release oral bioavailability 

Abbreviations

SMEDDS

Self-microemulsifying drug delivery system

PDI

Polydispersity index

MCC

Microcrystalline cellulose

HPMC

Hydroxypropyl methylcellulose

EC

Ethyl cellulose

HPLC

High-performance liquid chromatography

SR

Sustained release

IPM

Isopropyl myristate

GTCC

Caprylic capric triglyceride

EE

Encapsulation efficiency

Notes

Acknowledgments

The authors thank the University Ethics Committee for the kind guidance in the animal experiments.

Funding Information

This work was supported by the National Natural Science Foundation of China (81273470, 81473172, and 81503025), National “Twelfth Five-Year” Plan for Science & Technology Support (Grant 2013BAD16B07-1), Special Funds for 333 and 331 projects (BRA2013198), Indus-try University-Research Institution Cooperation (JHB2012-37, GY2012049, GY2013055) in Jiangsu Province and Zhenjiang City, Program for Scientific Research Innovation Team in Colleges and Universities of Jiangsu Province, and a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  1. 1.Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue EngineeringJiangsu UniversityZhenjiangPeople’s Republic of China
  2. 2.Jiangsu Provincial Research Center for Medicinal Function Development of New Food ResourcesZhenjiangPeople’s Republic of China
  3. 3.Tashkent State Agricultural University (Nukus branch)NukusUzbekistan
  4. 4.Jiangsu Tian Sheng Pharmaceutical Co., LtdZhenjiangPeople’s Republic of China
  5. 5.Key Laboratory of Drug Delivery & Tissue RegenerationZhenjiangPeople’s Republic of China

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