Formulation and evaluation of matrix microspheres for simultaneous delivery of salbutamol sulphate and theophylline

Purpose: The objective of this study was to formulate and evaluate a matrix microsphere system for simultaneous delivery of two anti-asthmatic drugs Salbutamol sulphate and Theophylline which are often indicated for the management of asthma, their frequent dosing may reduce compliance, thus making a prolonged release formulation necessary. Ethylcellulose was used as a retardant polymer and its compatibility with the drugs and the drug-drug compatibility were established through IR, XRD and DSC studies.
Method: Microspheres were prepared by emulsion solvent evaporation using acetone/light liquid paraffin system. Tween 80 was used as the dispersing agent and cyclohexane was added to harden the microspheres. The prepared microspheres were characterized for their micromeritic properties and drug loading, as well as by infrared spectroscopy (IR), differential scanning calorimetry (DSC), x-ray powder diffractometry (XRD) and scanning electron microscopy (SEM). The in vitro release studies were performed in pH 7.4, phosphate buffer.
Result: The prepared microspheres were white, free flowing and spherical in shape. The drug-loaded microspheres showed 67-91% of entrapment and release was extended upto 6 to 8 h. The infrared spectra, differential scanning calorimetry thermographs and XRD spectra all showed the stable character of both the drugs in the drug-loaded microspheres and revealed the absence of drug-polymer interactions. Scanning electron microscopy study revealed that the microspheres were spherical and porous in nature.
Conclusion: The matrix microspheres have a potential for the prolongation and simultaneous delivery of the anti asthmatic drugs (salbutamol and theophylline).

Keywords
Matrix microspheres, Salbutamol sulphate, Theophylline, Ethylcellulose, Emulsion solvent evaporation technique.