Current Issue : July - September Volume : 2017 Issue Number : 3 Articles : 5 Articles
Background: Resveratrol effects on the prevention and treatment of colon\ncancer have been well documented recently, but low solubility, rapid\nabsorption and metabolism of resveratrol limit its beneficial effects on colon\ncancer. Designing a formulation that enhances the solubility of resveratrol,\nprotects resveratrol from oxidation and isomerization, and delivers it to the\ncolon is a priority of food and drug industry. In this study, resveratrolpolyethylene\nglycol (PEG)-loaded pectin-chitosan polyelectrolyte complex\nwas designed as a colon targeted delivery system.\nMethods: The effects of adding PEG, ultra-sonication time, pH, and pectin to\nchitosan ratio were investigated on particle size, polydispersity index (PDI),\nzeta potential by particle size analyzer, and scanning electron microscopy\n(SEM). Encapsulation efficiency (EE), release of resveratrol in simulated\ngastrointestinal fluid, and different pHs were analyzed via High Performance\nLiquid Chromatography (HPLC). Antioxidant activity was measured by (2, 2-\ndiphenyl-1-picryl-hydrazyl-hydrate) DPPH free-radical method.\nResults: Results showed that colloidal stable micro-particles (725 �± 20 nm)\nwith PDI < 0.3 and zeta potential +27 �± 2 mV was formed in the ratio of 5:1\nof pectin to chitosan w/v % after a 10-min sonication. Encapsulation\nefficiency was 81 �± 7 %. The reduction of antioxidant activity of resveratrol\nloaded micro-particles after one month was less than 13%. Micro-particles\nreleased about 33% of resveratrol in the simulated gastric and intestinal fluids.\nConclusion: Two-thirds of the loaded resveratrol in Pectin-Chitosan complex\nreached colon. The developed system had enough specification for enriching\nfruit based drinks due to remarkable colloidal stability in the pH range of 3.5\nto 4.5....
Nano eye-drops are a new type of ophthalmic treatment with increased potency and reduced side effects. Compounds in conventional eye-drops barely penetrate into the eye because the cornea, located at the surface of eye, has a strong barrier function for preventing invasion of hydrophilic or large-sized materials from the outside. In this work, we describe the utility of nano eye-drops utilising brinzolamide, a commercially available glaucoma treatment drug, as a target compound. Fabrication of the nanoparticles of brinzolamide prodrug increases the eye penetration rate and results in high drug efficacy, compared with that of commercially available brinzolamide eye-drops formulated as micro-sized structures. In addition, the resulting nano eye-drops were not toxic to the corneal epithelium after repeated administration for 1 week. The nano eye-drops may have applications as a next-generation ophthalmic treatment....
Background: This work aimed to provide useful information on the incidence of the choice of formulation in semisolid\npreparations of iron-oxide nanoparticles (IONs). The appropriate analytical methods to assess the IONs physical\nstability and the effect of the semi-solid preparations on IONs human skin penetration were discussed. The physical\nstability of IONs (Dh = 31 Ã?± 4 nm; Ã?¶ = âË?â??65 Ã?± 5 mV) loaded in five semi-solid preparations (0.3% w/v), namely\nCarbopol gel (CP), hydroxyethyl cellulose gel (HEC), carboxymethylcellulose gel (CMC), cetomacrogol cream (Cet)\nand cold cream was assessed by combining DLS and low-field pulsed NMR data. The in vitro penetration of IONs was\nstudied using human epidermis or isolated stratum corneum (SC).\nResults: Reversible and irreversible IONs aggregates were evidenced only in HEC and CMC, respectively. IONs diffused\nmassively through SC preferentially by an intercellular pathway, as assessed by transmission electron microscopy.\nThe semi-solid preparations differently influenced the IONs penetration as compared to the aqueous suspension.\nCet cream allowed the highest permeation and the lowest retained amount, while cold cream and CP favored\nthe accumulation into the skin membrane.\nConclusion: Basic cutaneous semi-solid preparations could be used to administer IONs without affecting their permeation\nprofile if they maintained their physical stability over time. This property is better discriminated by low-field\npulsed NMR measurements than the commonly used DLS measurements....
Oral administration is a desirable alternative of parenteral administration due to the\nconvenience and increased compliance to patients, especially for chronic diseases that require\nfrequent administration. The oral drug delivery is a dynamic research field despite the\nnumerous challenges limiting their effective delivery, such as enzyme degradation, hydrolysis\nand low permeability of intestinal epithelium in the gastrointestinal (GI) tract. pH-Responsive\ncarriers offer excellent potential as oral therapeutic systems due to enhancing the stability of\ndrug delivery in stomach and achieving controlled release in intestines. This review provides a\nwide perspective on current status of pH-responsive oral drug delivery systems prepared\nmainly with organic polymers or inorganic materials, including the strategies used to overcome\nGI barriers, the challenges in their development and future prospects, with focus on technology\ntrends to improve the bioavailability of orally delivered drugs, the mechanisms of drug release\nfrom pH-responsive oral formulations, and their application for drug delivery, such as protein\nand peptide therapeutics, vaccination, inflammatory bowel disease (IBD) and bacterial\ninfections....
Background: Mucoadhesion is an important property that helps oral drug delivery system to remain attached with\nbuccal mucosa and hence to improve the delivery of the drug. The current study was designed to achieve the thiol\nmodification of Arabinoxylan (ARX) and to develop a mucoadhesive oral film for the improved delivery of tizanidine\nhydrochloride (TZN HCl).\nMethod: Synthesis of thiolated arabinoxylan (TARX) was accomplished by esterification of ARX with thioglycolic\nacid (TGA). TARX was further used for the development of mucoadhesive oral films which were prepared by using\na solvent casting technique. Formulation of the films was designed and optimized by using central composite\ndesign (CCRD), selecting TARX (X1) and glycerol (X2) as variables. Prepared film formulations were evaluated for\nmechanical strength, ex-vivo mucoadhesion, in-vitro drug release, ex-vivo drug permeation, surface morphology and\ndrug contents.\nResults: Thiolation of ARX was confirmed by fourier transform infra-red spectroscopy (FTIR) as a peak related to\nthiol group appeared at 2516 cmâË?â??1. The claim of successful thiolation of ARX was strengthened by the presence of\n2809.003 Ã?± 1.03 Ã?¼moles of thiol contents per gram of the polymer, which was determined by Ellmanââ?¬â?¢s reagent\nmethod. From the results, it was observed that the films were of satisfactory mechanical strength and mucoadhesiveness\nwith folding endurance greater than 300 and mucoadhesive strength 11.53 Ã?± 0.17 N, respectively. Reasonable drug\nretention was observed during in-vitro dissolution (85.03% cumulative drug release) and ex-vivo permeation (78.90%\ncumulative amount of permeated drug) studies conducted for 8 h. Effects of varying concentrations of both polymer\nand plasticizer on prepared mucoadhesive oral films were evaluated by ANOVA and it was observed that glycerol can\nenhanced the dissolution as well as permeation of the drug while TARX has opposite impact on these parameters.\nConclusion: In nutshell, TARX in combination with glycerolwas found to be suitable for the development of controlled\nrelease mucoadhesive oral films of TZN HCl....
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