The aim of this study is to design and evaluate metoprolol succinate sustained release (SR) matrix tablets employing a natural gum blend as the rate-retarder. Developing a tablet matrix utilizing ...locust bean gum (LBG), xanthan gum (XG), and guar gum (GG) was done to aid metoprolol succinate release over a 24-h period and help in once-daily dosage, reducing nocturnal episodes in hypertensive patients. In an effort to create a synergistic effect, attempts were made to combine commonly used natural gums, XG and GG, with LBG, which served as the primary release-retardant. The optimal way to formulate the tablet was studied using polymer blend ratios of 1:1, 1:3, 1:5, 1:1:1, 1:2:1 and 1.5:1.5:1. The same created polymer mix was used as the binding agent to prepare tablets utilizing the wet granulation process. Weight, thickness, hardness, content homogeneity, in-vitro drug release, erosion, and water uptake were used to characterize the formulations. Additional testing for drug-excipient compatibility was conducted. It was discovered that an XG:LBG:GG ratio of 1:2:1 produced the best outcomes having the highest t
75%
of cumulative drug release of 15.2 h, outperforming commercial formulations. A relation between the gum concentration and release rate retarding effect was also established. 3.33% of gum concentration showed optimal sustained release effects. The results concluded that the prepared SR metoprolol succinate tablets might be one of the best formulation for hypertensive patients that not only serves therapeutic purpose but also values the patients concern of providing minimal side-effect in the long run use of the medication.
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, SBNM, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
Our objective of this study is to design and develop a polyethylene glycol (PEG2000)-modified multiwall carbon nanotube (PEGylated MWCNT) formulation for oral controlled metronomic chemotherapeutic ...drug delivery. Multiwall carbon nanotubes undergo various chemical modifications including oxidation with strong acids, conjugation of polyethylene glycol, and coating with cellulose acetate phthalate which resulted in the formation of aqueous dispersion and prevention of drug degradation in acidic environment. Advanced analytical procedure such as Fourier transform infra-red, X-ray diffraction, differential scanning calorimetry, thermal gravimetric analysis, transmission electron microscopy, and dynamic light scattering techniques were used to evaluate physicochemical characterization. We also performed in vitro cytotoxic study by MTT assay and results revealed that carboplatin-loaded PEGylated MWCNTs did not show significant detrimental effect on the viability of MDA-MB-231 (human breast cancer) cells. The maximum encapsulation and drug-loading capacity were determined to be 71.58 ± 0.04 and 39.62 ± 0.07%, respectively. The release of carboplatin from PEGylated MWCNTs was investigated at simulated intestinal fluid (SIF), pH 6.8, after optimizing at simulated gastric fluid (SGF), pH 1.2, by enteric coating. Enteric-coated PEGylated MWCNTs exhibit pH-responsive drug activity in a sustained manner especially at pH 6.8. This surface modification strongly suggests that PEGylated MWCNTs could be a potential carrier for metronomic chemotherapeutic agent for high drug resistance, drug with maximum adverse effect and poorly oral bioavailable drugs.
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OBVAL, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, SBNM, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
3.
Niosome: A future of targeted drug delivery systems Kazi, Karim Masud; Mandal, Asim Sattwa; Biswas, Nikhil ...
Journal of advanced pharmaceutical technology and research,
10/2010, Volume:
1, Issue:
4
Journal Article
Peer reviewed
Open access
Over the past several years, treatment of infectious diseases and immunisation has undergone a revolutionary shift. With the advancement of biotechnology and genetic engineering, not only a large ...number of disease-specific biological have been developed, but also emphasis has been made to effectively deliver these biologicals. Niosomes are vesicles composed of non-ionic surfactants, which are biodegradable, relatively nontoxic, more stable and inexpensive, an alternative to liposomes. This article reviews the current deepening and widening of interest of niosomes in many scientific disciplines and, particularly its application in medicine. This article also presents an overview of the techniques of preparation of niosome, types of niosomes, characterisation and their applications.
Chitosan (CS) is one of the most functional natural biopolymer widely used in the pharmaceutical field due to its biocompatibility and biodegradability. These privileges lead to its application in ...the synthesis of nanoparticles for the drug during the last two decades. This article gives rise to a general review of the different chitosan nanoparticles (CSNPs) preparation techniques: Ionic gelation, emulsion cross-linking, spray-drying, emulsion-droplet coalescence method, nanoprecipitation, reverse micellar method, desolvation method, modified ionic gelation with radial polymerisation and emulsion solvent diffusion, from the point of view of the methodological and mechanistic aspects involved. The physicochemical behaviour of CSNPs including drug loading, drug release, particles size, zeta potential and stability are briefly discussed. This review also directs to bring an outline of the major applications of CSNPs in drug delivery according to drug and route of administration. Finally, derivatives of CSNPs and CS nano-complexes are also discussed.
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DOBA, IJS, IZUM, KILJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
Chitosan (CS) is one of the most successfully developed biodegradable polymers. Among the numerous polymers developed to formulate polymeric nanoparticles, CS has fascinated considerable attention ...due to its appealing properties: (i) biodegradability and biocompatibility, (ii) FDA approval for wound dressings as well as in dietary application, (iii) non-toxicity, (v) scope of sustained release, (vi) probability to modify surface properties and (vii) scope of target nanoparticles (NPs) to particular organs or cells. This review presents different preparation methods of chitosan nanoparticles (CSNPs) from the methodological and mechanistic point of view. The crosslinking agent including aldehyde, tripolyphosphate (TPP), genipin and other cross linkers and the physicochemical behaviour of CSNPs including drug loading, drug release, particles size, zeta-potential and stability are briefly discussed. This review also presents why CS has been chosen to design nanoparticles (NPs) as drug delivery systems in various pharmaceutical applications.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
To develop a pH responsive drug delivery system (DDS) for controlled release of therapeutic cargo, Doxazosin Mesylate (DZM) which was loaded into carrier material mesoporous silica nanoparticle (MSN) ...and subsequently coated with Eudragit S-100(ES-100) to release the drug at pH 7.4.
We have synthesized cylindrical MSN under acidic condition using non-ionic surfactant (Pluronic(®) P 123) and Tetraethoxysilane (TEOS). After post synthesis treatment (PST) surfactant was removed by calcination. To obtain pH sensitive release calcined MSN was coated with ES-100 (MSN-DZMES100). The Brauner-Emmett-Teller (BET) surface area, adsorption isotherm, t-plot, pore volume of MSN were done in surface area analyzer to characterize different MSN samples (as synthesized, calcined, and coated).
Highest surafce area (427.114 m(2)/g) was observed in case of calcined sample when compared to as synthesized (3.1198m(2)/g) and coated MSN (8.8480m(2)/g). Adsorption pore width of final coated sample was 12.58 nm whereas as synthesized and calcined samples possessed pore width 36.82 nm and 7.32 nm respectively. All uncoated and coated MSN samples were further characterized with FESEM, TEM, FTIR. No significant interaction between drug and MSN was found from FTIR studies. The drug loading into coated mesoporous support was found to be 43.7%. In vitro studies were done at different pH using Franz-diffusion cell. Results showed significant release at pH 7.4 from MSNDZM- ES100. Cumulative drug release over a period of 10 hr was 81% at this systemic pH.
ES-100 coated mesoporous silica nanoparticle is a smart carrier for pH responsive release of guest molecule.
The aim of this study was to characterize the provesicle formulation of nateglinide (NTG) to facilitate the development of a novel controlled release system of NTG with improved efficacy and oral ...bioavailability compared to the currently marketed NTG formulation (Glinate™ 60). NTG provesicles were prepared by a slurry method using the non-ionic surfactant, Span 60 (SP), and cholesterol (CH) as vesicle forming agents and maltodextrin as a coated carrier. Multilamellar niosomes with narrow size distribution were shown to be successfully prepared by means of dynamic laser scattering (DLS) and field emission scanning electron microscopy (FESEM). The absence of drug-excipient interactions was confirmed by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. In vitro release of NTG in different dissolution media was improved compared to pure drug. A goat intestinal permeation study revealed that the provesicular formulation (F4) with an SP:CH ratio of 5:5 gave higher cumulative amount of drug permeated at 48 h compared to Glinate™ 60 and control. A pharmacodynamic study in streptozotocin-induced diabetic rats confirmed that formulation F4 significantly (P<0.05) reduced blood glucose levels in comparison to Glinate 60. Overall the results show that controlled release NTG provesicles offer a useful and promising oral delivery system for the treatment of type II diabetes.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Novel drug delivery system using nanoscale materials with a broad spectrum of applications provides a new therapeutic foundation for technological integration and innovation. Nanoparticles are ...suitable drug carrier for various routes of administration as well as rapid recognition by the immune system. Gelatin, the biological macromolecule is a versatile drug/vaccine delivery carrier in pharmaceutical field due to its biodegradable, biocompatible, non-antigenicity and low cost with easy availability. The surface of gelatin nanoparticles can be modified with site-specific ligands, cationized with amine derivatives or, coated with polyethyl glycols to achieve targeted and sustained release drug delivery. Compared to other colloidal carriers, gelatin nanoparticles are better stable in biological fluids to provide the desired controlled and sustained release of entrapped drug molecules. The current review highlights the different formulation aspects of gelatin nanoparticles which affect the particle characteristics like zeta potential, polydispersity index, entrapment efficacy and drug release properties. It has also given emphasis on the major applications of gelatin nanoparticles in drug and vaccine delivery, gene delivery to target tissues and nutraceutical delivery for improving the poor bioavailabity of bioactive phytonutrients.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
Innovation in the delivery system is a key tool for increasing the bioavailability of active pharmaceutical ingredients (API). The oral route is the most promising and convenient route of drug ...administration over the years. However, the delivery of proteinaceous drugs poses a serious issue in this regard. Enzymes’ ability to break down proteins demands other routes of administration. Trans Dermal Delivery Systems (TDDS) mediated by microneedles have demonstrated notable outcomes in this instance. Transdermal administration avoids first-pass metabolism and enables long-term drug release. Microneedle drug administration is a more contemporary technique for proteinaceous drug delivery that avoids first-pass metabolism and is less intrusive and painful than the parenteral route. Recent studies have shown that MNs, which are essentially micron-sized needles of a few hundred nm in diameter, may be made using biodegradable polymers. The amount of toxicity has been minimised because to the use of biodegradable materials in the production of microneedles. Larger proteinaceous drugs, however, have trouble penetrating the body. The combination of physical enhancement techniques with it and the creation of a novel tool have increased drug penetration, which has in turn drastically altered the preexisting situation. So, the method created could be a useful technique to distribute different protein molecule types and aid in the delivery of diverse proteinaceous therapeutics. This review provides an in-depth look at the aforementioned situation and discusses numerous studies on the application of various biopolymers that have demonstrated significant effects in this regard as well as physical enhancing methods to increase skin permeability, such as thermal ablation, sonophoresis, and electroporation.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Purpose
Glimepiride, an anti-diabetic and third-generation sulfonylurea drug belonging to class II BCS (Biopharmaceutical Classification System) type, is characterized by its low solubility and high ...permeability. In order to increase glimepiride’s aqueous solubility and hence increase its dissolution rate, the goal of this study was to formulate the drug as binary and ternary solid dispersion employing water-soluble carriers.
Methods
Three binary solid dispersions of glimepiride were prepared by solvent evaporation technique using β-cyclodextrin with different drug carrier ratios. After optimizing the binary solid dispersion concerning solubility improvement, four different ratios of ternary solid dispersion employing polyvinylpyrrolidone K30 (PVPK30) were fabricated with the optimized solid dispersion to determine solubility and compared with marketed formulation to determine the consequence of the study. Further FTIR, XRD, and DSC studies were performed for a better understanding of the characterization of optimized solid dispersion and to know if there are any significant interactions with water-soluble carriers or with excipients.
Results
The combination of the glimepiride and β-cyclodextrin systems significantly increases the solubility and in the case of ternary solid dispersion, the solubility is increased even more. The enhancement of the solubility is influenced by the carrier’s concentration.
Conclusions
A total of four tablet formulation batches that were prepared and the explicit in vitro comparisons been carried out with commercially available immediate-release formulation, suggested that formulating glimepiride in ternary solid dispersion has enhanced the solubility and dissolution rate drastically.
Graphical Abstract
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, SBNM, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
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