Improvement in dissolution rate and photodynamic efficacy of chlorin e6 by sucrose esters as drug carrier in nanosuspension formulation: optimisation and in vitro characterisation

Shubhajit Paul, Paul Wan Sia Heng, Lai Wah Chan

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

Objectives: Chlorin e6 is a poorly water-soluble photoactive drug. Its monomers form aggregates at the tumour physiological pH, which drastically reduces its photodynamic efficacy. This study aimed to improve the dissolution rate and photodynamic efficacy of chlorin e6 by nanosuspension formulation using biodegradable sucrose esters as drug carrier. Methods: A modified emulsion-solvent diffusion method was used to prepare the nanosuspension, where amount of Ce6, ratio of sucrose monopalmitate to sucrose monolaurate as carrier and ratio of dichloromethane to acetone as solvent, were varied using central composite design. Particle size, zeta potential, encapsulation efficiency and in vitro drug release characteristics of the nanosuspensions were evaluated. The formulation was optimised by response surface methodology and its photodynamic efficacy evaluated. Key findings: The optimised nanosuspension had mean particle size of ~200 nm, 88% drug encapsulation efficiency and faster drug release compared to pure Ce6. Spectroscopic studies showed that Ce6 exists in monomeric form in the carrier, which facilitated a remarkable increase in cellular uptake, in vitro singlet oxygen generation and cytotoxicity to oral squamous carcinoma cells. Conclusions: The dissolution rate and photodynamic efficacy of Ce6 were markedly improved by formulating the drug as a nanosuspension with sucrose esters as drug carrier.

Original languageEnglish (US)
Pages (from-to)1152-1163
Number of pages12
JournalJournal of Pharmacy and Pharmacology
Volume70
Issue number9
DOIs
StatePublished - Sep 2018

Bibliographical note

Funding Information:
This research was supported by the Singapore Ministry of Health’s National Medical Research Council under IRG NMRC/1187/2008 (R-148-000-114-213) and GEA-NUS PPRL fund (N-148-000-008-001).

Publisher Copyright:
© 2018 Royal Pharmaceutical Society

Keywords

  • Ce6
  • dissolution
  • nanosuspension
  • photodynamic efficacy
  • sucrose-esters-carrier

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