A review on chitosan and its nanocomposites in drug delivery.

How to investigate drug use in health facilities : selected drug use indicators

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Buccal films of ondanstron hydrochloride were fabricated from mucoadhesive polymer, chitosan, and polyvinyl pyrrolidone (PVP K30) for the purpose of prolonging drug release and improving its bioavailability. All fabricated film formulations prepared were smooth and translucent, with good flexibility. The weight and thickness of all the formulations were found to be uniform. Drug content in the films ranged from 98 - 99%, indicating favorable drug loading and uniformity. The inclusion of PVP K30, a hydrophilic polymer, significantly reduced the bioadhesive strength and in vitro mucoadhesion time of the films, although the degree of swelling increased. In vitro drug release studies in simulated saliva showed a prolonged release of over five to six hours for all formulations, except C4, with 99.98% release in 1.5 hours. Kinetic analysis of the release data indicated that the best fit model with the highest correlation coefficient for all formulations was the Peppas model. In vivo studies, on selected films in rabbits, were conducted, to determine the pharmacokinetic parameters such as C(max), T(max), and AUC(0-∞), using model-independent methods with nonlinear least-squares regression analysis. The AUC and values of C(max) of ondansetron hydrochloride were found to be significantly greater (P < 0.005) than the selected films C2 and C3, as compared to those from the oral solution, thereby confirming improved bioavailability via the buccal route. The T(max) values were also significantly greater (P < 0.005), indicating the slower release of the drug from buccal films, thereby, providing prolonged effects. Good in vitro-in vivo correlation was observed with R(2) values exceeding 0.98, when the percentage of drug released was correlated with the percentage of drug absorbed.

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In vitro and in vivo evaluation of chitosan buccal films of ondansetron hydrochloride

Purpose: This study was designed to develop and evaluate chitosan films containing ciprofloxacin and diclofenac sodium for the topical treatment of periodontitis. Methods: Chitosan films containing ciprofloxacin alone and in combination with diclofenac sodium were prepared by solvent casting method. Some of the drug-loaded films were crosslinked with 2% gluteraldehyde for 2 and 4 h, respectively. The films were then evaluated for their physicochemical properties including weight variation, thickness, tensile strength, in vitro release, stability and antibacterial activity. Results: Mean weight and thickness data showed that the different films were uniform. Tensile strength was maximum for drug-free films and minimum for films containing the highest amount of drug(s). In vitro drug release data indicate that the films showed an initial burst release followed by sustained release of the drug(s). Films stored at refrigerated conditions exhibited slower degradation rate. The drug-loaded films that were crosslinked for 4 h had inhibitory effect on Staph mutans for up to 24 days. Conclusion: The study suggests that crosslinked chitosan film containing ciprofloxacin and diclofenac is a potential drug delivery device for the topical treatment of periodontitis. Good physicochemical properties were shown by the films.

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Formulation of chitosan-based ciprofloxacin and diclofenac film for periodontitis therapy

The current study was aimed to develop an amphiphilic drug-lipid nano-complex of rutin:egg phosphatidylcholine (EPC) to enhance its poor absorption and bioavailability, and investigated the impact of the complex on hepatoprotective and antioxidant activity. Rutin nano-complexes were prepared by solvent evaporation, salting out and lyophilisation methods and compared for the complex formation. For the selected lyophilisation method, principal solvent DMSO, co-solvent (t-butyl alcohol) and rutin:EPC ratios (1:1, 1:2 and 1:3) were selected after optimisation. The properties of the nano-complexes such as complexation, thermal behaviour, surface morphology, molecular crystallinity, particle size, zeta potential, drug content, solubility, in vitro stability study, in vitro drug release, in vitro and in vivo antioxidant study, in vivo hepatoprotective activity and oral bioavailability/pharmacokinetic studies were investigated. Rutin nano-complexes were developed successfully via the lyophilisation method and found to be in nanometric range. Rutin nano-complexes significantly improved the solubility and in vitro drug release, and kinetic studies confirmed the diffusion-controlled release of the drug from the formulation. The nano-complex showed better antioxidant activity in vitro and exhibited well in vitro stability in different pH media. The in vivo study showed better hepatoprotective activity of the formulation compared to pure rutin at the same dose levels with improved oral bioavailability. Carbon tetrachloride (CCl4)-treated animals (group II) failed to restore the normal levels of serum hepatic marker enzymes and liver antioxidant enzyme compared to the nano-complex-treated animals. The results obtained from solubility, hepatoprotective activity and oral bioavailability studies proved the better efficacy of the nano-complex compared to the pure drug.

Nano-lipid Complex of Rutin: Development, Characterisation and In Vivo Investigation of Hepatoprotective, Antioxidant Activity and Bioavailability Study in Rats

Tetracycline is a broad spectrum antimicrobial agent, which is formulated into films and evaluated for the treatment of periodontitis. Chitosan films containing tetracycline in three different concentrations (10, 20, and 30% w/w to the weight of polymer) were prepared by the solution casting method, using 1% v/v acetic acid solution. The prepared films were evaluated for various properties such as weight variation, tensile strength, stability studies, in-vitro release, and mass balance studies. Further films were cross-linked in order to extend the drug release. Average weight and thickness among the different films was uniform.Tensile strength was maximum for plain films and minimum for films containing the highest percentage of the drug or cross-linked films. The stability studies did not show any significant changes. Static dissolution studies showed a burst release initially followed by a progressive fall in the release of the drug, and also showed extended release when cross-linking was attempted. The in-vitro release kinetics of tetracycline followed the zero order pattern. The fact that the mass balance studies done after in-vitro dissolution did not deviate by more than 3% from the experimental drug content, confirms that the drug is in free form rather than bound to the polymer.

R Narayana Charyulu

Papers

In vitro and in vivo evaluation of chitosan buccal films of ondansetron hydrochloride

Formulation of chitosan-based ciprofloxacin and diclofenac film for periodontitis therapy

Nano-lipid Complex of Rutin: Development, Characterisation and In Vivo Investigation of Hepatoprotective, Antioxidant Activity and Bioavailability Study in Rats

Formulation and in-vitro evaluation of Chitosan films containing tetracycline for the treatment of periodontitis

Etched ion track polymer membranes for sustained drug delivery