T he aim of the present investigation is to develop and evaluate transdermal patches of nebivolol. The transdermal patches of nebivolol were prepared by solvent evaporation technique. Twelve formulations of nebivolol patches were prepared that composed of ethyl cellulose (EC) with hydroxyl propyl methyl cellulose (HPMC) and ethyl cellulose with polyvinyl pyrrolidine (PVP) in different ratios of 1:2, 1:4, 1:6, 2:1, 4:1, and 6:1 w/w, as film former. Polyvinyl alcohol (4% w/v) was used to prepare the backing membrane. All formulations contained Tween 80 (4% v/w) as penetration enhancer and propylene glycol (40% v/w) as plasticizer in dimethyl formamide as solvent system. The prepared transdermal patches of nebivolol were evaluated for thickness, mass variation, drug content, moisture content, moisture vapor transmission, folding endurance, tensile strength, ex vivo drug permeation study, drug release kinetics, scanning electron microscopy, primary skin irritancy study, and stability study. The physicochemical interactions between nebivolol and different polymers were studied by Fourier Transform Infrared (FTIR). The maximum drug release in 24 h was 95.185% (T2, HPMC:EC is 1:4), which is significant (P < 0.05). Furthermore, the formulation T2 showed maximum skin permeation (13.93 mg/cm 2 /h) in comparison with other formulations. The mechanical properties and tensile strength revealed that the formulations were found to be strong enough but not brittle. FTIR studies did not show any evidence of interaction between the drug and the polymers. Nebivolol matrix-type transdermal therapeutic systems could be prepared with the required flux having suitable mechanical properties.
In the present study, Glipizide, a drug mainly preferred for type-II diabetes, is formulated in the form of floating mucoadhesive tablets to improve its bioavailability. Hydroxy Propyl Methyl Cellulose K200M, Sodium Carboxy Methyl Cellulose, Carbopol 974P, Karaya gum, Chitosan, and Xanthan gum were used as mucoadhesive polymers in designing of the floating mucoadhesive tablets. Different proportions of glipizide and polymer were used to prepare tablets. Pre-compression evaluation studies evaluated the powder blend of Glipizide mucoadhesive tablets (Pre-compression blend). It concluded that the blend had good flow property and better compressibility by interpreting the data obtained from the test. Hence the floating mucoadhesive tablets were prepared by direct compression technique. The results of floating lag time, and buoyancy studies suggested that formulations had a satisfactory floating ability. The release profile of the active pharmaceutical ingredient (glipizide) from the prepared dosage form indicated a controlled and enhanced drug release for a period of 12hrs. An in-vivo study done for selected formulation. By the interpretation of data obtained from all the evaluation studies (Pre-compression test, floating property, drug release profile, & in-vivo study) concluded that formulation GF8 containing drug: Carbopol 974P (1:2) was optimized. The drug release kinetics of the formulation GF8 followed the Higuchi model with a regression value of 0.993.
In this present study, floating mucoadhesive tablets of Rosiglitazone were formulated to improve the gastric retention time and overall bioavailability. Different mucoadhesive polymers like HPMC K200 M, Na CMC, Carbopol 974P, Karaya gum, Chitosan and Xanthan gum were selected to formulate the tablets. Various formulations were prepared by using these polymers in different concentration. The pre-compression blend of Rosiglitazone mucoadhesive tablets were characterized with respect to angle of repose, bulk density, tapped density, carr’s index and hausner’s ratio and all the results indicated that the blend was having good flow property and hence better compression properties. The swelling studies were performed for the formulations and the results depicted that all the formulations have a good swelling index. The drug release studies depicted that the formulations release the drug in first order. So based on the results, formulation RF13 was found to be an optimized formulation. Keywords: Mucoadhesive tablets, Rosiglitazone, Bioadhesive polymers.
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