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Nano Composite Emulsion for Sustained Drug Release and Improved Bioavailability

Pharmaceutical Research volume 31, pages 2774–2783 (2014)Cite this article

ABSTRACT

Purpose

To propose a novel composite nanoemulsion formulation that contains no surfactant, but offers great stability and improved oral absorption capabilities.

Methods

The nanoemulsions were prepared by dispersing the oil phase into aqueous solutions containing different amounts of the PMMA/silica composite nanoparticles. The stability was tested under extreme conditions. The structure features of the nanoemulsion droplets were investigated using Electron microscope. The in vitro drug release and in vivo drug absorption profiles after oral administration were investigated using Cyclosporin A as a model drug.

Results

The composite nanoemulsion demonstrated great stability under various disruptive conditions. Electron microscopy studies indicated the existence of internal and surface domains in the nano-droplet structure. In vitro drug release and in vivo uptake characterizations also confirmed the unique interfacial properties of such nanoemulsion structures.

Conclusions

The novel nanoemulsion formulation may have modulated drug release profiles and alternative oral absorption mechanisms, which could offer significant advantages compared to traditional emulsion formulations.

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Abbreviations

CMC:

Critical micellar concentration

CNC:

Cellulose Nanocrystals

ddH2O:

Double distilled H2O

EM:

Electronic Microscopy

IR:

Infrared Spectroscopy

MALT:

Mucosal associate lymph tissue

NCE:

New chemical entity

PDI:

Polydispersity Index

P-gP:

P-glycoprotein

PMMA:

Polymethyl Methacrylate

PTA:

Phosphotungstic Acid

SEDDS:

Self-emulsifying drug delivery system

SGF:

Simulated gastric fluids

SIF:

simulated intestinal fluids

SMEDDS:

Self-microemulsifying drug delivery system

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ACKNOWLEDGMENTS AND DISCLOSURES

This study was supported by grants from NSF China No. 81273465.

Wenqiang Sun and Xinrui Ma contributed equally to this work and should be considered co-first authors.

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Affiliations

  1. School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Rd, Shanghai, 200240, People’s Republic of China

    Wenqiang Sun, Xinrui Ma, Xiaohui Wei & Yuhong Xu

Authors
  1. Wenqiang Sun
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  2. Xinrui Ma
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  3. Xiaohui Wei
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  4. Yuhong Xu
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Correspondence to Yuhong Xu.

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Sun, W., Ma, X., Wei, X. et al. Nano Composite Emulsion for Sustained Drug Release and Improved Bioavailability. Pharm Res 31, 2774–2783 (2014). https://doi.org/10.1007/s11095-014-1374-7

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  • DOI: https://doi.org/10.1007/s11095-014-1374-7

KEY WORDS

  • cyclosporin A
  • nano composite emulsion
  • oral bioavailability
  • physical stability
  • poorly soluble drugs