Development of the composition of the dry nasal spray vinpocetine and the technology of its production

Introduction. Vinpocetine has neuroprotective properties and is used to improve cognitive function; however, poor solubility and low bioavailability may limit its use. The development of a dry nasal spray vinpocetine with increased solubility is a topical issue.

Aim of the study was to develop the composition of a prototype dry nasal spray of vinpocetine and the technology for its production.

Material and Methods. The prototypes contained chitosan and synthesized poly-β-cyclodextrin. The formation of host-guest inclusion complexes by co-dissolution and co-attrition methods increased vinpocetine solubility. IR spectroscopy and X-ray diffraction analysis were used to confirm the formation of inclusion complexes and evaluate the sample properties. Spray drying was the final step in the formation of the dry nasal spray. The stability and mass (volume) uniformity of doses taken from a multi-dose package, dosing in a dry powder dispenser, and in vitro permeability in a transdermal diffusion tester were studied for the lead formulation.

Results. Comparative studies of the developed samples with different vinpocetine:polycyclodextrin ratios were conducted. No significant differences in inclusion complex formation were demonstrated by the two methods. Therefore, the co-dissolution method was chosen as the preferred method for producing dry nasal spray prototype samples, as it is technologically simpler. In vitro permeation results showed that most of the vinpocetine dissolves and penetrates the membrane within 30 minutes. Dosage uniformity and stability of the developed prototypes for 12 months were demonstrated.

Conclusions. The experimental studies demonstrate the feasibility of using powder particles containing the vinpocetine-polycyclodextrin inclusion complex and chitosan, obtained by spray drying, as prototypes for a dry nasal spray for vinpocetine.