ABSTRACT
Abstract The goal of the present study was to develop inclusion complexes and polymers dispersions of ramipril prepared by physical mixing, kneading, co-evaporation, and solvent evaporation methods to enhance drug solubility and dissolution rate, and thereby to reduce drug dose and side effects using selected hydrophilic carriers such as β-CD, PVP-K25, PEG 4000, and HPMC K100M. The prepared formulations were characterized for solubility and in-vitro drug release studies. The systematic optimization of formulations was performed using I-Optimal experimental design by selecting factors such as type of carriers (X1), drug: carrier ratio (X2), and method of preparation (X3), and response variables including percent yield (Y1), solubility (Y2), Carr's index (Y3) and drug release in 30 min (Y4). Mathematical modeling was carried out using a quadratic polynomial model. The inclusion complex formulation (F27) was selected as an optimized batch by numerical desirability function and graphical optimization with the help of design space. The inclusion complex prepared by the co-evaporation method showed maximum drug solubility and released in pH 6.8 phosphate buffer compared to pure and other formulations. The inclusion complex is a feasible approach to improve the solubility, dissolution rate, bioavailability, and minimization of drugs' gastrointestinal toxicity upon oral administration of ramipril.
ABSTRACT
SUMMARY Blepharitis is a common chronic eye condition that causes eyelid inflammation, leading to inflamed, irritated, sticky and itchy eyelids and flaking of the skin. For its treatment, patients often need indefinite use of an eyelid cleaning solution which usually cost more than 20 USD per 80 ml bottle and lasts, on average, one month. For those patients unable to afford the treatment, physicians recommend the use of a do it yourself (DIY) solution. However, the efficacy of DIY eyelid solutions might fluctuate according to the type of blepharitis present in the patient and inadequate pH stabilization of the solution might promote additional itchiness, irritation, and dryness of the skin and eyes. Thus, we propose an optimized DIY solution prototype for symptom management in patients with chronic blepharitis. The formulation contains a significant ratio of tea tree oil and resulted in suitable pH and foam expansion values. The low cost and ease of preparation of the designed formulation make it an affordable, effective alternative in the treatment of chronic blepharitis.
RESUMEN La blefaritis crónica es una condición ocular que causa inflamación en los párpados, dando como resultado párpados irritados, pegadizos y descamación de la piel. Pacientes con esta condición necesitan usualmente de la aplicación de una solución de limpieza de párpados que cuesta en promedio 20 USD por cada 80 ml de solución y tiene un rendimiento de un mes. Para aquellos pacientes incapaces de costear el tratamiento, los médicos recomiendan el uso de soluciones hazlo tú mismo (DIY en inglés). Sin embargo, la eficacia de estas en el tratamiento de la condición puede fluctuar de acuerdo con el tipo de blefaritis presente. Adicionalmente, una inadecuada estabilización del pH de la solución puede promover una mayor irritación, resequedad y picazón en la piel y en los ojos. Por lo tanto, en este trabajo proponemos un prototipo experimental de solución DIY para el manejo sintomático de pacientes con blefaritis crónica. La formulación contiene una proporción significativa de aceite de árbol de té y posee un pH adecuado y alta producción de espuma para su correcta aplicación en la piel. El bajo costo y facilidad de preparación hacen de ella una alternativa efectiva y asequible en el tratamiento de la blefaritis crónica.