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      Proniosomal Telmisartan Tablets: Formulation, in vitro Evaluation and in vivo Comparative Pharmacokinetic Study in Rabbits

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          Abstract

          Objective

          The purpose of this study was to prepare proniosomal vesicles of Telmisartan (TEL) to be compressed into tablets which will be further evaluated in vitro and in vivo.

          Materials and Methods

          An experimental design was adopted using surfactants of different HLB values (span 40-brij 35), different cholesterol ratios (20–50%) and different phospholipid types (egg yolk-soyabean). Different responses were measured followed by tablet manufacturing. The highest EE was shown in F3 (85%) while the lowest value was obtained in F7 (8.4%). Finally, zeta potential results were in the range of −0.67 to −27.6 mv. Compressibility percent revealed that F5 showed an excellent flowability characteristic with a value of 9.74±1.61 while F3 and F6 showed good flowability characteristics. By the end of the release, F6 showed approximately 90% drug release.

          Results

          F6 was selected for the in vivo study; C max was increased by 1.5-fold while AUC 0-∞ also increased significantly by 3-fold when compared with commercial tablet and finally, t max was increased by 3-fold indicating sustained release pattern. The relative bioavailability was also increased by 3.2-fold.

          Conclusion

          The results of this study suggested that the formulation of compressed tablets containing more stable proniosomal powder extended the release of TEL and increased its bioavailability as well.

          Related collections

          Most cited references 31

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          Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs.

          Poor water solubility of many drugs has emerged as one of the major challenges in the pharmaceutical world. Polymer-based amorphous solid dispersions have been considered as the major advancement in overcoming limited aqueous solubility and oral absorption issues. The principle drawback of this approach is that they can lack necessary stability and revert to the crystalline form on storage. Significant upfront development is, therefore, required to generate stable amorphous formulations. A thorough understanding of the processes occurring at a molecular level is imperative for the rational design of amorphous solid dispersion products. This review attempts to address the critical molecular and thermodynamic aspects governing the physicochemical properties of such systems. A brief introduction to Biopharmaceutical Classification System, solid dispersions, glass transition, and solubility advantage of amorphous drugs is provided. The objective of this review is to weigh the current understanding of solid dispersion chemistry and to critically review the theoretical, technical, and molecular aspects of solid dispersions (amorphization and crystallization) and potential advantage of polymers (stabilization and solubilization) as inert, hydrophilic, pharmaceutical carrier matrices. In addition, different preformulation tools for the rational selection of polymers, state-of-the-art techniques for preparation and characterization of polymeric amorphous solid dispersions, and drug supersaturation in gastric media are also discussed.
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            Biophysical aspects of using liposomes as delivery vehicles.

             Anne S Ulrich (2002)
            Liposomes are used as biocompatible carriers of drugs, peptides, proteins, plasmic DNA, antisense oligonucleotides or ribozymes, for pharmaceutical, cosmetic, and biochemical purposes. The enormous versatility in particle size and in the physical parameters of the lipids affords an attractive potential for constructing tailor-made vehicles for a wide range of applications. Some of the recent literature will be reviewed here and presented from a biophysical point of view, thus providing a background for the more specialized articles in this special issue on liposome technology. Different properties (size, colloidal behavior, phase transitions, and polymorphism) of diverse lipid formulations (liposomes, lipoplexes, cubic phases, emulsions, and solid lipid nanoparticles) for distinct applications (parenteral, transdermal, pulmonary, and oral administration) will be rationalized in terms of common structural, thermodynamic and kinetic parameters of the lipids. This general biophysical basis helps to understand pharmaceutically relevant aspects such as liposome stability during storage and towards serum, the biodistribution and specific targeting of cargo, and how to trigger drug release and membrane fusion. Methods for the preparation and characterization of liposomal formulations in vitro will be outlined, too.
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              Enhanced bioavailability of silymarin by self-microemulsifying drug delivery system.

              The main purpose of this study was to prepare lipid-based self-microemulsifying drug delivery system (SMEDDS) to improve peroral bioavailability of silymarin. SMEDDS was a system consisting of silymarin, Tween 80, ethyl alcohol, and ethyl linoleate. Particle size change of the microemulsion was evaluated upon dilution with aqueous media and loading with incremental amount of silymarin. In vitro release was investigated by a dialysis or an ultrafiltration method. Results showed that release of silymarin from SMEDDS was limited, incomplete, and typical of sustained characteristics. Pharmacokinetics and bioavailability of silymarin suspension, solution, and SMEDDS were evaluated and compared in rabbits. Plasma silybin, which was treated as the representing component of silymarin, was determined by high-performance liquid chromatography. After gavage administration of silymarin suspension, plasma silybin level was very low and fell below limit of detection 4h after. As for silymarin solution and SMEDDS, double peak of maximum concentrations were observed, which was characteristic of enterohepatic circulation. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 1.88- and 48.82-fold that of silymarin PEG 400 solution and suspension, respectively. It was concluded that bioavailability of silymarin was enhanced greatly by SMEDDS. Alternative mechanisms, such as improved lymphatic transport pathway, other than improved release may contribute to enhancement of bioavailability of silymarin.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                DDDT
                dddt
                Drug Design, Development and Therapy
                Dove
                1177-8881
                31 March 2020
                2020
                : 14
                : 1319-1331
                Affiliations
                [1 ]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University , Cairo, Egypt
                [2 ]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Horus University , New Damietta, Egypt
                [3 ]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Sinai University , North Sinai, Egypt
                [4 ]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Fayoum University , Fayoum, Egypt
                Author notes
                Correspondence: Mahmoud Hasan Teaima Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University , Cairo, EgyptTel +20 1005840264 Email mahmoud.teaima@pharma.cu.edu.eg
                Article
                245013
                10.2147/DDDT.S245013
                7127815
                © 2020 Teaima et al.

                This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

                Page count
                Figures: 7, Tables: 5, References: 34, Pages: 13
                Categories
                Original Research

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