Microparticles for drug delivery across mucosa and the blood-brain barrier

A mixture consisting of 273.6 mg of water, 16.4 mg of phosphatidylcholine, 20.0 mg of butanol, 32.0 mg of sodium taurocholate, 2.4 mg of butyric acid and 2.8 mg of dipalmitoyl phosphatidyl ethanolamine-PEG (steric stabilizer), warmed at 70.degree. C., is added under stirring to 52.0 mg of the water / oil microemulsion of the step b) of the Example 1.

The preparation is completed according to the steps d) and e) of the Example 1.

The following results are obtained:

drug incorporated in the microparticles: 78%;

average diameter of the microparticles: 100 nm;

polydispersion index: 0.24.

a) A mixture consisting of 24 mg of stearic acid and 6.0 mg of monostearine is warmed at 70.degree. C.;

b) a mixture consisting of 6.0 mg of gentamicin, 56.0 mg of sodium taurocholate, 28.0 mg of soy-bean phosphatidylcholine and 280.0 mg of water, warmed at 70.degree. C., is added under stirring to the mixture of the step a) obtaining an oil in water microemulsion.

The microemulsion obtained in the step b) is then treated as described in the steps d) and e) of the Example 1.

The following results are obtained:

gentamicin incorporated in the microparticles: 80%;

average diameter of the microparticles: 105 nm;

polydispersion index: 0.22.

a) A mixture consisting of 210.0 mg of stearic acid, 10.0 mg of monostearine, 62.0 mg of soy-bean phosphatidylcholine, 80.0 mg of butyric acid and 6.0 mg of butanol is warmed at 70.degree. C.

b) 36.0 mg of an aqueous solution of calcitonin (2 mg / ml) warmed at 68.degree. C. are added to the mixture of the step a) obtaining a water / oil microemulsion.

c) A mixture consisting of 214.4 mg of water, 16.8 mg of soy-bean phosphatidylcholine, 16.4 g of butyric acid, 8.0 g of butanol and 32.4 g of sodium taurocholate, warmed at 70.degree. C., is added under stirring to 52.0 mg of the water / oil microemulsion of the step b), obtaining a water / oil / water microemulsion.

The preparation is then completed working according to the steps d) and e) of the Example 1.

The following results are obtained:

incorporation of the calcitonin: 83%;

average diameter of the microparticles: 93 nm;

polydispersion index: 0.23.