Optimization of drug loading to improve physical stability of paclitaxel-loaded long-circulating liposomes

Vinayagam Kannan, Pavan Balabathula, Murali K. Divi, Laura Thoma, George C. Wood

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

The effect of formulation and process parameters on drug loading and physical stability of paclitaxel-loaded long-circulating liposomes was evaluated. The liposomes were prepared by hydration-extrusion method. The formulation parameters such as total lipid content, cholesterol content, saturated-unsaturated lipid ratio, drug-lipid ratio and process parameters such as extrusion pressure and number of extrusion cycles were studied and their impact on drug loading and physical stability was evaluated. A proportionate increase in drug loading was observed with increase in the total phospholipid content. Cholesterol content and saturated lipid content in the bilayer showed a negative influence on drug loading. The short-term stability evaluation of liposomes prepared with different drug-lipid ratios demonstrated that 1:60 as the optimum drug-lipid ratio to achieve a loading of 1-1.3 mg/mL without the risk of physical instability. The vesicle size decreased with an increase in the extrusion pressure and number of extrusion cycles, but no significant trends were observed for drug loading with changes in process pressure or number of cycles. The optimization of formulation and process parameters led to a physically stable formulation of paclitaxel-loaded long-circulating liposomes that maintain size, charge and integrity during storage.

Original languageEnglish (US)
Pages (from-to)308-315
Number of pages8
JournalJournal of Liposome Research
Volume25
Issue number4
DOIs
StatePublished - Oct 2 2015

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Paclitaxel
Liposomes
Lipids
Pharmaceutical Preparations
Pressure
Cholesterol
Phospholipids

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Optimization of drug loading to improve physical stability of paclitaxel-loaded long-circulating liposomes. / Kannan, Vinayagam; Balabathula, Pavan; Divi, Murali K.; Thoma, Laura; Wood, George C.

In: Journal of Liposome Research, Vol. 25, No. 4, 02.10.2015, p. 308-315.

Research output: Contribution to journalArticle

Kannan, Vinayagam ; Balabathula, Pavan ; Divi, Murali K. ; Thoma, Laura ; Wood, George C. / Optimization of drug loading to improve physical stability of paclitaxel-loaded long-circulating liposomes. In: Journal of Liposome Research. 2015 ; Vol. 25, No. 4. pp. 308-315.
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