New pharmaceutical microemulsion system for encapsulation and delivery of diospyrin, a plant-derived bioactive quinonoid compound.
A new vegetable oil based oil-in-water microemulsion is developed and characterized as a prospective delivery system for in vivo application A particular weight percent composition 5/30/65 (clove oil/Tween-20/water) was selected (V1) from the clear oil-in-water zone of the pseudoternary phase diagram comprising clove oil, polyoxyethylene sorbitan monolaurate (Tween-20), and water. Two modifications of V1, (V2 and V3) were prepared by addition of dipalmitoyl phosphatidyl choline (DPPC), and a mixture of DPPC and cholesterol, respectively. A model drug diospyrin (a plantderived quinonoid compound) was encapsulated in the dispersed clove oil droplets of the three systems and designated as DV1, DV2, and DV3, respectively. The size of the dispersed clove oil droplets ranged between 9-20 nm as determined by dynamic light scattering. The stability of the vehicles, before and after encapsulation, was assessed under varying conditions of time and temperature and was found to be stable for 1 year and over a temperature range of 4-40 degrees C. The ultraviolet-visible spectrum of diospyrin after encapsulation in the compartmentalized medium remained almost identical to that dissolved in chloroform. The single-dose acute toxicity of V1 and DV1 was assessed in vivo by carrying out survival study and enzyme assay in Swiss Albino mice. The vehicle was safe at a volume of 0.05 ml when injected intraperitoneally into the mice.
Centre for Surface Science, Department of Chemistry, Jadavpur University, Kolkata, India. syamasri@yahoo.com
Syamasri
S
Gupta
S P
SP
Moulik
Banasri
B
Hazra
Rekha
R
Ghosh
S K
SK
Sanyal
S
S
Datta
D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry; D000469:Alkaline Phosphatase / Q000097:blood; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000633:toxicity; D002784:Cholesterol / Q000737:chemistry; D045783:Clove Oil / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry / Q000633:toxicity; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D051379:Mice; D009285:Naphthoquinones / Q000008:administration & dosage* / Q000633:toxicity; D010316:Particle Size; D044367:Phase Transition; D011136:Polysorbates / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D023382:Toxicity Tests, Acute / Q000379:methods; D000637:Transaminases / Q000097:blood; D014867:Water / Q000737:chemistry
D000970:Antineoplastic Agents; D045783:Clove Oil; D004655:Emulsions; D009285:Naphthoquinones; D011136:Polysorbates; D014867:Water; D015060:1,2-Dipalmitoylphosphatidylcholine; D002784:Cholesterol; D000637:Transaminases; D000469:Alkaline Phosphatase; C043546:diospyrin