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

Research output: Contribution to journalArticle

19 Citations (Scopus)

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

Fingerprint

Inbred C57BL Mouse
Liposomes
Melanoma
Half-Life
Particle Size
Pharmaceutical Preparations
Antineoplastic Agents
plumbagin
Pharmacokinetics
Phosphates
Lipids
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Sunil Kumar, M. R. ; Kiran Aithal, B. ; Udupa, N. ; Sreenivasulu Reddy, M. ; Raakesh, V. ; Murthy, R. S.R. ; Prudhvi Raju, D. ; Satish Rao, B. S. / 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. In: Drug Delivery. 2011 ; Vol. 18, No. 7. pp. 511-522.
@article{0e7f80a98b9a415fb8c80160291c358d,
title = "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",
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.",
author = "{Sunil Kumar}, {M. R.} and {Kiran Aithal}, B. and N. Udupa and {Sreenivasulu Reddy}, M. and V. Raakesh and Murthy, {R. S.R.} and {Prudhvi Raju}, D. and {Satish Rao}, {B. S.}",
note = "cited By 12",
year = "2011",
month = "9",
doi = "10.3109/10717544.2011.595840",
language = "English",
volume = "18",
pages = "511--522",
journal = "Drug Delivery",
issn = "1071-7544",
publisher = "Informa Healthcare",
number = "7",

}

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

In: Drug Delivery, Vol. 18, No. 7, 09.2011, p. 511-522.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Formulation of plumbagin loaded long circulating pegylated liposomes: In vivo evaluation in C57BL/6J mice bearing B16F1 melanoma

T2 - In vivo evaluation in C57BL/6J mice bearing B16F1 melanoma

AU - Sunil Kumar, M. R.

AU - Kiran Aithal, B.

AU - Udupa, N.

AU - Sreenivasulu Reddy, M.

AU - Raakesh, V.

AU - Murthy, R. S.R.

AU - Prudhvi Raju, D.

AU - Satish Rao, B. S.

N1 - cited By 12

PY - 2011/9

Y1 - 2011/9

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=80052932440&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=80052932440&partnerID=8YFLogxK

U2 - 10.3109/10717544.2011.595840

DO - 10.3109/10717544.2011.595840

M3 - Article

C2 - 21793763

AN - SCOPUS:80052932440

VL - 18

SP - 511

EP - 522

JO - Drug Delivery

JF - Drug Delivery

SN - 1071-7544

IS - 7

ER -