Formulation of plumbagin loaded long circulating pegylated liposomes: In vivo evaluation in C57BL/6J mice bearing B16F1 melanoma: In vivo evaluation in C57BL/6J mice bearing B16F1 melanoma

M. R. Sunil Kumar, B. Kiran Aithal, N. Udupa, M. Sreenivasulu Reddy, V. Raakesh, R. S.R. Murthy, D. Prudhvi Raju, B. S. Satish Rao

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Abstract

Context and Objective: Plumbagin (2-methyl, 5-hydroxy, 1, 4-naphthoquinone), an anticancer agent is encapsulated either as conventional or long circulating liposomal formulations to enhance its biological half-life and antitumor efficacy. Methods: The liposomes were prepared by thin film hydration method and in vitro characterization was carried out to examine the particle size, zeta potential, drug encapsulation efficiency and in vitro release. The optimized formulations were tested for pharmacokinetic and pharmacodynamic efficacy against mice bearing B16F1 melanoma. Also in vivo toxicity studies were carried out. Results and Discussion: The optimum particle size and entrapment efficiency was observed at drug to lipid molar ratio of 1:20. The in-vitro release of plumbagin from the liposomal formulations in phosphate-buffered saline (pH 7.4) showed biphasic release with an initial burst release followed by sustained release phase. Elimination half life (T1/2) of pegylated, conventional and free plumbagin was 1305.76±278.16, 346.87±33.82 and 35.89±7.95min respectively. Further, plumbagin exhibited better antitumor efficacy in vivo when administered as long circulating liposomes with no signs of normal tissue toxicity. Conclusion: It can be concluded that the pegylated liposomes could provide a promising parenteral platform for plumbagin with enhanced plasma half-life and therapeutic efficacy.

Original languageEnglish
Pages (from-to)511-522
Number of pages12
JournalDrug Delivery
Volume18
Issue number7
DOIs
Publication statusPublished - 09-2011

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All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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