Chitosan-coated poly(є-caprolactone) nanocapsules for mucoadhesive applications of perillyl alcohol

ABSTRACT

Perillyl alcohol (POH) is an essential oil found in several plants and presents significant therapeutic and chemo-preventive activity against some tumors. However, it exhibits low aqueous solubility and thereby reduced oral absorption and bioavailability. Nanoencapsulation of POH can be an important tool to overcome such limitations. In this work, chitosan was used for coating poly (ε-caprolactone) nanocapsules for mucoadhesive applications of POH. The nanocapsules were obtained by the nanoprecipitation method and presented a mean diameter of about 330 nm, spherical morphology, polydispersity index of 0.14, zeta potential of +32 mV, and POH encapsulation efficiency of 56%. POH was prolonged released from nanocapsules. In mucoadhesion studies, nanocapsules showed higher adsorption to mucin compared to free POH, possibly due to electrostatic interactions between chitosan and mucin. In the cytotoxicity assay, POH-loaded nanocapsules presented higher IC₅₀ than free POH; however, they were more selective for HT-29 tumor cells than for normal Vero cells. The results demonstrate the potential application of chitosan-coated nanocapsules for the oral administration of POH intended for cancer therapy.

KEYWORDS:

• Perillyl alcohol
• nanocapsules
• poly(ε-caprolactone)
• chitosan
• mucin

Acknowledgments

The authors thank the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES-Brazil) for the scholarship for L. Penteado, COMCAP-UEM (Complex of Research Support Centers), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq-Brazil), PRONEX/Fundação Araucária (Brazil), and Financiadora de Projetos e Estudos (FINEP-Brazil) for partial financial support.

Additional information

Funding

This work was supported by the CNPq; Coordenação de Aperfeiçoamento de Pessoal de Nível Superior [001]; Financiadora de Estudos e Projetos; Fundação Araucária.