For systemic drug delivery, the buccal region offers an attractive route of drug administration. Salbutamol sulfate is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It's oral bioavailability is ∼40% due to extensive first pass metabolism. Salbutamol sulfate patches were prepared using Eudragit L-100, HPMC, PVA and Carbopol 934 in various proportions and combinations using PEG-400/PG as plasticizers. Patches were laminated on one side with a water impermeable backing layer for unidirectional drug release. The thickness of medicated patches were ranged between 0.23 ± 0.008 and 0.59 ± 0.007 mm and mass varied between 65.23 ± 3.3 and 117.92 ± 4.2 mg. Patches showed an increase in mass and swelling index with PEG-400 when compared with PG. The surface-pH of patches ranged between 6 and 7. Formulations E7 (7.5 mL Eudragit L-100, 15 mL HPMC K4M, 7.5 mL PVA and 2 mL PEG-400), E12 (7.5 mL Eudragit L-100, 7.5 mL PVA, 15 mL Carbopol and 2 mL PEG-400), F7 (7.5 mL Eudragit L-100, 15 mL HPMC K4M, 7.5 mL PVA and 2 mL PG), and F12 (7.5 mL Eudragit L-100, 7.5 mL PVA, 15 mL Carbopol and 2 mL PG) showed high folding endurance. Residence time of the tested patches ranged between 101 and 110 min. The maximum in vitro release was found to be 99.93% over a period of 120 min for formulation F12. Data of in vitro release from patches were fitted to different kinetic models such as Higuchi and Korsmeyer-Peppas models to explain the release profile. Formulations E7 and F7 were best fitted to the non-Fickian, where as formulations E12 and F12 showed Fickian/anomalous drug release. Stability studies indicated that there was no change in the chemical and physical characteristics during the test period.

Antihyperglycemic and hypolipidemic effects of ethanol extract of aerial parts of Melothria maderaspatana and Coccinia indica were evaluated in STZ induced diabetes in Sprague–Dawley rats. The rats were concurrently treated with 100 or 200 mg/kg b.w. p.o. for 14 days. The changes in fasting blood glucose level and body weight were measured in 5 days interval. After 14 days experimental period, rats were sacrificed by cervical decapitation, blood and liver samples were collected. Biochemical estimation of plasma glucose, cholesterol, triglycerides, LDL, HDL, SGOT, SGPT and ALP were done from blood sample. The liver glycogen content was estimated using standard procedure from homogenized liver sample. Administration of EEMm or EECi to STZ-diabetic rats caused significant antihyperglycemic and hypolipidemic effects (p < 0.001). The extracts were also found to be significantly effective (p < 0.001; p < 0.05) on recovery of altered biochemical parameters and decreased body weight in treated animals. Glibenclamide (0.5 mg/kg b.w.) was used as standard in present study.

Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery: Buccal patches of salbutamol sulfate were prepared using five different water soluble polymers in various proportions and combinations using PEG-400/PG as plasticizers. A 3² full factorial design was used to design the experiments for each polymer combination. Patches were laminated on one side with a water impermeable backing layer for unidirectional drug release. The thickness of medicated patches ranged between 0.2 and 0.4 mm and showed an increase in mass whenever PEG-400 was used as plasticizer. The surface pH of all patches approached neutral. Eight formulations which had shown high folding endurance (> 300) were selected for evaluation. Patches prepared with PEG-400 showed a high swelling index. The residence time of the tested patches ranged between 105 and 130 min. Formulations A10, A32, B10 and B32 fitted the Higuchi model best, whereas formulations A19 and B19 showed super case II transport drug release. Stability studies indicated that there was no change in the chemical and physical characteristics during the test period of 6 months.

Abstract: Mucoadhesive buccal patches of Salbutamol Sulphate were prepared using five different polymers (polyvinyl pyrrolidone [PVP]), polyvinyl alcohol [PVA], water soluble chitosan [CHWS], acid soluble chitosan [CHAS], hydroxypropyl methyl cellulose [HPMC]) in various proportions and combinations (CHWS/PVP/HPMC, CHWS/PVA/HPMC, CHAS/PVP/HPMC, and CHAS/PVA/HPMC). A 32 full factorial design was used to design the experiments. A total of 72 patches were prepared. Thickness of the patches ranged between 0.3±0.003 and 0.6±0.009 mm. Mass of the patches were in the range of 68.12±4.6 to 95.52±5.0 mg. Patches showed increased mass whenever PEG -400 was used as plasticizer. The surface pH of patches were acidic to neutral (pH 4-pH 7). Patches showed satisfactory drug loading efficiency (85% to 97%). Eight formulations (C9, C18, C27, C36, D9, D18, D27 and D36)-which showed high folding endurance- were selected for further characterization. Patches with PEG -400 showed higher swelling index when compared to PG. The residence time of the patches ranged between 115 min and 120 min. Formulation C18 showed the maximum in vitro drug release of 101.4 % over a period of 120 min. Formulations D36 and C36 were best fitted to Higuchi model. The remaining formulations were best fitted to the Korsmeyer-Peppas model. Drug permeation was fast and showed the similar profile as that of the in vitro drug release. Patches were stable, during and at the end of the accelerated stability study.