in vitro release

The present investigation was aimed to develop Glipizide loadedproliopsomal carrier system for Transdermal drug delivery which, deliver the drug effectively over an extended period of time to improve the anti diabetic effect of the loaded drug. Glipizide loaded proliposomal  gel was prepared by coacervation-phase separation method using different combinations of drug, sorbitol with cholesterol and lecithin (GF1 – GF6). Proliposome formulations were characterized for physical appearance, pH, vesicle size, entrapment efficiency, drug content uniformity, surface morphology, zeta potential analysis, in-vitro drug release, skin irritation test, and hypoglycemic activity. Among the different formulation, GF2 formulation showed more entrapment efficiency and drug content compared to all other formulations.  The optimized formulation GF4 showed maximum reduction in blood glucose level 101.83 ± 0.983at 24 hrs as compared to oral drug. Proliposomal gel (PLG1) showed no skin irritation and delivered the Glipizide in a controlled manner as compared to conventional dosage form, as evidenced by a significant decrease in blood glucose level in diabetes rats. Thus proliposomal gel will be suitable drug delivery system for Glipizide due to ease of preparation and incorporation of less number of excipients.

  Promethazine Hydrochloride (PMZ), a low bioavailabe drug, used for the management of emesis. The purpose of the present investigation was to develop buccoadhesive tablets for PMZ and to evaluate for their physicochemical, in vitro, ex vivo and in vivo parameters. Ex vivo drug permeation through porcine buccal membrane from the drug solution was conducted to know the permeation characteristics of the PMZ. The controlled-release PMZ tablets were produced by direct compression method using Sodium CMC and Carbopol 934P as mucoadhesive polymers and evaluated for in vitro drug release, in vitro bioadhesion, in vivo residence time, swelling and erosion studies, surface pH, ex vivo drug permeation through porcine buccal membrane from the optimized buccal tablet (F10) and stability studies. Formulation F10 showed maximum drug release (96.3 %) in 6 h, with the Higuchi model release profile and permeated 49.8 % of the drug with flux 1.45 mg h–1cm–2 through porcine buccal membrane. The optimized formulation showed peak detachment force (1.64 N), work of adhesion (0.36 mJ), in vivo residence time (287 min), swelling index (204%), erosion (53.1%) and surface pH (6.92). In vivo mucoadhesive behaviour of the optimized formulations was studied in healthy human volunteers and subjective parameters were evaluated. The stability of the optimized formulation was studied and no significant changes were detected in drug content and in vitro release after 6 months. PMZ mucoadhesive tablets for buccal delivery could be prepared with required permeation, bioadhesive and in vivo residence properties.