Formulation and investigation of lacidipine as a nanoemulsions

Abstract EN

Lacidipine (LCDP) is a calcium-channel blocker with low aqueous solubility and bioavailability.

Nanoemulsion (NE) is one of the popular methods that has been used to solve the solubility problems of many drugs.

LCDP was formulated as a NE utilizing triacetin as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant.

Nine formulas were prepared, and different tests performed to ensure the stability of the NEs, such as thermodynamic stability, particle size, polydispersity index, zeta potential, dilution test, conductivity test, drug content, viscosity and in-vitro drug release.

Results of characterization showed that LCDP NE (F-5) using triacetin, tween80, ethanol and DDW in a ratio of (10: 60: 30) was selected as the best formula, since it has excellent thermodynamic stability with a particle size of 13.

42, low PDI 0.

234, zeta potential (-14.

5mV), good dilution without drug precipitation, efficient electrical conductivity 0.

241ms/cm, higher percent of drug content (99.

14%) with acceptable viscosity, and complete release of the drug after (30 min.

) with significantly higher (P<0.

05) dissolution rate in comparison with pure drug powder.

The selected formula (F-5) subjected to further investigations as drug and excipient compatibility study by Fourier transform infrared spectroscopy (FTIR) and high performance liquid chromatography (HPLC) and Atomic force microscope (AFM).

The outcomes of the (FTIR) explain that the distinctive peaks for LCDP were displayed the same functional group's band with very slight shifting, which suggests the presence of hydrogen bonding.

This indicates that there was no interaction between LCDP and other NE components, while the HPLC demonstrated that was no change in retention time and no extra peaks reported.

Therefore, these excipients were found to be compatible with LCDP.

In conclusion, the NE was found to be an efficient method to enhance the solubility and dissolution rate of drugs that have poor water solubility (lipophilic drugs).