OBJECTIVETo investigate the influence of drug properties on the encapsulation effiency (EE) and drug release of transfersomes for a proper transfersome preparation.

METHODTo prepare the transfersomes of colchicines (CLC), vincristine sulfate (VCR) and mitoxantrone hydrochloride (DHAD) with the same materials and methods, and then measure their EE. To find out the relationship between drug properties like solubility, molecular weight and charges, and EE. To performe the drug release experiments of various types of transfersomes in vitro, and compare their differences.

RESULTVCR and DHAD are lipophilic or hydrophilic, owing positive charges and large molecular weight, as a result, their EE are high, while CLC is amphipathic, neutral, and of small molecular weight, its EE is very low. As DHAD can insert into the membrane of transfersome, the drug release of DHAD-T in vitro is much slower than that of VCR-T.

CONCLUSIONTo prepare transfersomes with high EE, drugs that are lipophilic or hydrophilic, high molecular weight and opposite charges to the membrane should be chosen. Interaction between drugs and membrane will influnce the rate of drug release.

Antineoplastic Agents ; administration & dosage ; chemistry ; Antineoplastic Agents, Phytogenic ; administration & dosage ; chemistry ; Colchicine ; administration & dosage ; chemistry ; Deoxycholic Acid ; Drug Carriers ; Gout Suppressants ; administration & dosage ; chemistry ; Mitoxantrone ; administration & dosage ; chemistry ; Particle Size ; Phosphatidylcholines ; Solubility ; Technology, Pharmaceutical ; methods ; Vincristine ; administration & dosage ; chemistry

The aim of this study was to observe the effects of uric acid lowering therapy (UALT), febuxostat and allopurinol, on blood pressure (BP) and serum creatinine level. Post-hoc data were derived from a phase-III, randomised, double-blind, 4-week trial of male gouty patients that compared the safety and efficacy of febuxostat and allopurinol in adults with gout. The subjects were randomly assigned to one of five groups, 35-37 in each group (febuxostat: 40, 80, 120 mg/d; allopurinol: 300 mg/d; control group: placebo). Blood pressure and serum creatinine level were measured at baseline and at weeks 2 and 4. Diastolic BP and creatinine level had decreased significantly in the UALT groups compared to the control group at week 4. Diastolic BP had decreased significantly in the allopurinol group and serum creatinine level had decreased significantly in the febuxostat groups at week 4. After adjusting for confounding variables, serum uric acid changes were found to be significantly correlated with changes in serum creatinine level but were not associated with changes in systolic or diastolic BP. UALT in gouty subjects significantly decreased diastolic BP and serum creatinine level. Changes in uric acid were significantly correlated with those in serum creatinine level, suggesting the feasibility of renal function improvement through UALT in gouty men.
Allopurinol/*administration & dosage ; Biological Markers/blood ; Blood Pressure/*drug effects ; Creatinine/*blood ; Dose-Response Relationship, Drug ; Gout/*drug therapy ; Gout Suppressants/administration & dosage ; Humans ; Hypertension, Renal/diagnosis/etiology/*prevention & control ; Male ; Middle Aged ; Reproducibility of Results ; Sensitivity and Specificity ; Thiazoles/*administration & dosage ; Treatment Outcome