Development of Mesalazine Microspheres for Colon Targeting

Abstract

Objective: The present work was aimed at preparation of mesalazine microspheres by a non-aqueous solvent evaporation method using eudragit S 100 and eudragit L 100 as pH dependent polymers for colon targeting. Methods:The ratio of drug to polymer was varied and the effect of formulation variables revolutions per minute (RPM) (1000, 1500, 2000 and 2500) and concentration of span 80 (1%, 1.5%, 2% and 2.5%) were studied. Prepared microspheres were evaluated for particle size, percent drug entrapment, granular analysis, in vitro drug release studies, Fourier transformed infrared spectroscopy (FT-IR) Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) studies.Results: Particle size has decreased and percent drug entrapment had increased with increase in RPM in all formulations. When the span 80 concentration increased, the particle size of the microsphere formulations increased and percent drug entrapment decreased in eudragit S 100 microspheres; whereas in eudragit L 100 microspheres, as the concentration of span 80 increased, the particle size of the microsphere formulations decreased. The prepared microspheres sustained the drug release over a period of 12 h. Conclusion:Thus eudragit S 100 and eudragit L 100 microspheres could constitute a promising approach for colon-specific and sustained delivery of mesalazine for the treatment of inflammatory bowel disease.

Design, Formulation and Evaluation of Liposome Containing Isoniazid

“…Differential Scanning Calorimetry (DSC) thermograms were taken by scanning the samples of (i) pure isoniazid, (ii) excipients containing (lecithin, cholesterol) and (iii) the formulation (F1 and F6) using DSC (Pyris Diamond TG/DTA, PerkinElmer, SINGAPORE) in nitrogen atmosphere (150 ml/min). Platinum crucibles were used with alpha alumina powder as reference [8,16].…”

Formulation and in Vitro Evaluation of Ramelteon Tablets for Colon Drug Delivery System by Compression Coating

“…The matrices of polysaccharides are assumed to remain intact in the physiological environment of the stomach and small intestine, but once they reach in the colon, they are acted upon by the bacterial polysaccharides and results in the degradation of the matrices. A large number of polysaccharides such as amylose, guar gum, pectin, chitosan, inulin, cyclodextrins, chondroitin sulphate, dextrans, dextrin and locust bean gum have been investigated for their use in colon targeted drug delivery systems [4,5]. The most important fact in the development of polysaccharide derivatives for colon targeted drug delivery is the selection of a suitable biodegradable polysaccharide.…”

Porous Plastic Matrix Tablets of Levetiracetam for Zero-Order Controlled Release: Development and Formulation Optimization

“…Drugs with high solubility as well as high dose require a high amount of polymer for achieving controlled release which may greatly increase the final weight of the tablet thus causing difficulty in swallowing. Though several technologies like different matrix and reservoir systems [1][2][3] have been investigated to address this challenge, still there is a significant scope to investigate further especially by employing highly hydrophobic polymers like plastic matrices [4][5][6]. Adequate literature published the use of plastic polymers like Eudrgait and other hydrophobic matrices to attain the controlled release drug release some of them include were by Apurba Sarker Apu et al [7]; H Tabandeh et al [8]; Sarika Pundir et al [9]; and Sudarshan Singh et al [10].…”