Formulation Development and Evaluation of Colon Targeted Microspheres for The Delivery of Poorly Soluble Drug (Parecoxib)

Abstract

Parecoxib, an injectable pro drug of valdecoxib, has shown superior analgesic activity in patients with postoperative dental pain and similar to ketorolac 30 or 60 mg. It also showed greater analgesic activity in gynecological and orthopaedic surgery. It is well-tolerated after surgery and produces fewer gastrointestinal erosions and ulcers than ketorolac. The study aims to develop colon-targeted microspheres for poorly soluble drugs, focusing on improving bioavailability, patient compliance, reducing dosing frequency, minimizing side effects, optimizing microsphere size and shape, selecting suitable polymers, and evaluating drug release profiles.The study focuses on the preparation of Sodium alginate, Aloe vera gel powder, and Almond gum powder microspheres using the iconic gelation method. Variables like drug: polymer ratio, glutaraldehyde concentration, and cross-linking time were optimized using a factorial design. The microspheres showed good in vitro mucoadhesion (88-96%) and no aggregation between drug and polymer. The results suggest promising potential for delivering Active Pharmaceutical Ingredients and could be an alternative to conventional dosage forms.