scholarly journals Calcium Alginate-Neusilin US2 Nanocomposite Microbeads for Oral Sustained Drug Delivery of Poor Water Soluble Drug Aceclofenac Sodium

2015 ◽  
Vol 2015 ◽  
pp. 1-14 ◽  
Author(s):  
Manjanna Kolammanahalli Mallappa ◽  
Rajesh Kesarla ◽  
Shivakumar Banakar
Keyword(s):  
Drug Release ◽  
Calcium Alginate ◽  
Crosslinking Agent ◽  
Phosphate Buffer Solution ◽  
Water Soluble ◽  
Gelling Agent ◽  
Simulated Gastric Fluid ◽  
Buffer Solution ◽  
Simulated Intestinal Fluid ◽  
Neusilin Us2

The aim of the present study was to formulate and investigate the calcium alginate- (CA-) Neusilin US2 nanocomposite microbeads containing preconcentrate of aceclofenac sodium (ACF-Na) liquid microemulsion (L-ME) for enhancement of oral bioavailability. The preconcentrate L-ME is prepared by using Labrafac PG, Labrasol, and Span 80 as oil, surfactant, and cosurfactant, respectively. The solid CA nanocomposite microbeads of L-ME prepared by microemulsification internal gelation technique using sodium alginate (SA) gelling agent, Neusilin US2 as adsorbent, and calcium chloride as crosslinking agent. L-ME has good thermodynamic stability; globule size was found to be 32.4 nm with polydispersity index 0.219 and −6.32 mV zeta potential. No significant interactions of excipients, drug in the formulations observed by FT-IR, DSC and XPRD. The concentration of SA and Neusilin US2 influences the flow properties, mean particle size, mechanical strength, drug entrapment efficiency, and percentage of drug release. All the formulations show minimum drug release in simulated gastric fluid (SGF) pH 1.2 for initial 2 h, maximum drug release in pH 6.8 phosphate buffer solution (PBS) at 6 h, followed by sustaining in simulated intestinal fluid (SIF) of pH 7.4 up to 12 h. The interaction of SA with Neusilin US2 creates a thick thixotropic gel network structure which acts as barrier to control the release of drug in the alkaline pH environment. Neusilin US2 is a novel filler used to convert L-ME into solid nanocomposite microbeads to enhance dissolution rate of poor water soluble drugs sustaining the drug release for prolonged period of time.

Synthesis of N-Carboxymethyl Chitosan Beads for Controlled Drug Delivery Applications

2006 ◽  
Vol 514-516 ◽  
pp. 1015-1019 ◽  
Author(s):  
Rangasamy Jayakumar ◽  
Rui L. Reis ◽  
João F. Mano
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Phosphate Buffer Solution ◽  
Controlled Drug Delivery ◽  
Gastric Fluid ◽  
Carboxymethyl Chitosan ◽  
Water Soluble ◽  
Buffer Solution ◽  
Chitosan Beads

N-Carboxymethyl chitosan (NCMC) is a water soluble derivative of chitosan. The NCMC beads were prepared by using ionotropic gelation process with the counter polyanion tripolyphoshate at pH 4.0 and characterized by scanning electron microscopy. The swelling behavior of the beads at different time intervals was monitored at different pH conditions. The in vitro drug release behavior in various pH solutions was studied using indomethacin as a model drug with two different concentrations (0.3 and 0.6% w/w). The release percent of indomethacin from NCMC beads was found to increase with increasing of pH in phosphate buffer solution medium due to the ionization of carboxymethyl group and high solubility of indomethacin in alkaline medium. These results indicated that the NCMC beads are useful for controlled drug delivery systems through oral administration by avoiding the drug release in the highly acidic gastric fluid region of the stomach.

Drug Release Behaviors of a pH/Temperature Sensitive Hydrogel Bead with Core-Shelled Structure

2010 ◽  
Vol 148-149 ◽  
pp. 1427-1430 ◽  
Author(s):  
Kui Lin Deng ◽  
Li Rong Dong ◽  
Yu E Shi ◽  
Yu Bo Gou ◽  
Qian Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Phosphate Buffer Solution ◽  
Temperature Sensitive ◽  
Buffer Solution ◽  
Hydrogel Bead ◽  
The Core ◽  
Drug Delivery Carrier ◽  
Temperature Sensitive Hydrogel ◽  
Biomedical Fields

As a drug delivery carrier, a novel pH/temperature sensitive bead (pTSB) with core-shelled structure from poly(N-acryloylglycine) (PAG), copoly(N-acryloylglycine methyl este and N-acryloylglycine ethyl ester) was prepared by two steps. In pH=7.4 phosphate buffer solution (PBS), the cumulative release amount of indomethacin loaded in the pTSB was about 60.1 % within 500 mins, but this value only reached to 22.3 % in pH=2.1 PBS. The release behaviors of indomethacin from pTSB also exhibited a remarkable dependence on PAG content in the core. Additionally, the release rate of indomethacin was much faster at 18 oC than that at 37 oC due to the temperature sensitivity of poly(N-acryloylglycinates). The experimental results indicate that pTSB seems to have a potential application in the drug release system controlled via pH or temperature in the biomedical fields.

Drug-loaded ultrafine poly(vinyl alcohol) fibre mats prepared by electrospinning

e-Polymers ◽  
2005 ◽  
Vol 5 (1) ◽  
Author(s):  
Chunxue Zhang ◽  
Xiaoyan Yuan ◽  
Lili Wu ◽  
Jing Sheng
Keyword(s):  
Drug Release ◽  
Photoelectron Spectroscopy ◽  
Vinyl Alcohol ◽  
Phosphate Buffer Solution ◽  
Poly Vinyl Alcohol ◽  
High Porosity ◽  
Buffer Solution ◽  
Drug Molecules ◽  
Alcohol Fibre

AbstractSubmicron poly(vinyl alcohol) (PVA) fibre mats embedded with Aspirin and bovine serum albumin (BSA) were prepared by electrospinning of their aqueous solutions. Fibre morphology was investigated by scanning electron microscopy. The composition of the fibre mats was characterized by Fourier transform IR spectroscopy and X-ray photoelectron spectroscopy. The in vitro drug release was investigated by immersing the fibre mats in phosphate buffer solution at 37°C. Results indicated that the morphology of fibre mats was influenced by the amount of drug, and more beaded and irregularly shaped fibres were found with increasing drug amounts. There were drug molecules distributed on the surface of the PVA fibres. Studies of in vitro drug release showed that both Aspirin and BSA were released more quickly from PVA fibre mats than from PVA films because of the large surface area and high porosity of the fibre mats.

Design and In-Vivo Evaluation of Risperidone Buccal Mucoadhesive Patches of Interpolymer Matrix

2021 ◽  
pp. 5305-5312
Author(s):  
Pradeep HK ◽  
Girish B ◽  
Nooruddeen K ◽  
Thimmasetty J ◽  
Venkateswarlu BS
Keyword(s):  
Drug Release ◽  
Drug Absorption ◽  
Kinetic Models ◽  
Phosphate Buffer Solution ◽  
Water Soluble ◽  
Content Uniformity ◽  
Human Beings ◽  
Insoluble Polymers

The buccal cavity is an alternate route for the administration of the drug. This route gained acceptance as increase in bioavailability is observed due to bypass of first pass metabolism. Solvent casting method was employed for the preparation of the risperidone mucoadhesive patches using different combinations of water soluble and water insoluble polymers using polyvinyl alcohol as a backing layer. Our main objective of this study was to understand the behaviour of water soluble and water insoluble polymers in combination on release pattern. Six different formulations of mucoadhesive patches were evaluated for physicochemical parameters like weight uniformity, content uniformity, thickness uniformity, surface pH, swelling studies, tensile strength, folding endurance, in-vitro drug release, and in-vivo drug absorption. Drug loaded mucoadhesive patches of various polymer bases had shown 35.64 to 72.33% drug release in 30 min in phosphate buffer solution of pH 6.6. In-vitro release data from patches were fit to different equations and kinetic models to explain release profiles. Kinetic models like Hixon-Crowell and Higuchi models were used. The formulation containing HPMC (15Cps) and polyvinyl pyrrolidone was considered as optimized based on the physicochemical and pharmaceutical properties. In-vivo studies in rabbits, carried out with prior permission from IAEC, showed 80.40% of drug release from the optimized patches. In-vivo and in-vitro correlations were found to be good. The drug absorption was found significant from the optimized formulation in healthy rabbits. The structure of the buccal membrane and permeability factors are similar in both human beings and rabbits. Therefore mucoadhesive patches of risperidone may be accepted with the important advantage of reduced risperidone dose.

scholarly journals Carbon-Based Magnetic Nanocarrier for Controlled Drug Release: A Green Synthesis Approach

2018 ◽  
Vol 5 (1) ◽  
pp. 1 ◽  
Author(s):  
Jessica Oliveira ◽  
Raquel Rodrigues ◽  
Lillian Barros ◽  
Isabel Ferreira ◽  
Luís Marchesi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Magnetic Nanoparticles ◽  
Drug Release ◽  
Phosphate Buffer ◽  
Colloidal Stability ◽  
Ph Dependence ◽  
Phosphate Buffer Solution ◽  
Controlled Drug Release ◽  
Buffer Solution ◽  
Carbon Based

In this study, hydrophilic magnetic nanoparticles were synthesized by green routes using a methanolic extract of Rubus ulmifolius Schott flowers. The prepared magnetic nanoparticles were coated with carbon-based shell for drug delivery application. The nanocomposites were further chemically functionalized with nitric acid and, sequentially, with Pluronic® F68 (CMNPs-plur) to enhance their colloidal stability. The resulting material was dispersed in phosphate buffer solution at pH 7.4 to study the Doxorubicin loading. After shaking for 48 h, 99.13% of the drug was loaded by the nanocomposites. Subsequently, the drug release was studied in different working phosphate buffer solutions (i.e., PB pH 4.5, pH 6.0 and pH 7.4) to determine the efficiency of the synthesized material for drug delivery as pH-dependent drug nanocarrier. The results have shown a drug release quantity 18% higher in mimicking tumor environment than in the physiological one. Therefore, this study demonstrates the ability of CMNPs-plur to release a drug with pH dependence, which could be used in the future for the treatment of cancer "in situ" by means of controlled drug release.

scholarly journals THE USE OF CLINOPTILOLITES AS CARRIER OF METFORMIN HYDROCHLORIDE IN DRUG DELIVERY SYSTEM: IN VITRO DRUG RELEASE STUDY

2018 ◽  
Vol 11 (11) ◽  
pp. 285
Author(s):  
Putra Imwa ◽  
Kusumawati Igaw
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Simulated Intestinal Fluid ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
N2 Sorption ◽  
Metformin Hcl

Objective: As an antidiabetic drug, metformin hydrochloride (HCl) has been well known to possess low oral bioavailability and short half-life. In this study, we prepared the drug delivery system (DDS) of metformin HCl and clinoptilolite as its carrier. The in vitro drug release profile was further investigated.Methods: DDS was made by encapsulating metformin HCl on clinoptilolite using the wet impregnation method at various pH and initial concentration of metformin HCl. Fourier transform infrared spectrometer (FTIR), X-ray diffractometer (XRD), and N2 Sorption Analyzer were used to characterize the as-synthesized DDS. Drug release study was conducted by stirring the DDS in simulated gastric fluid and simulated intestinal fluid over 12 h.Results: The encapsulation process was achieved optimally at pH 7.0 and initial concentration of metformin HCl of 300 mg/l (CLI2-300 denoted DDS). The results of FTIR and N2 sorption analyzer confirmed the existence of metformin HCl on clinoptilolites. Meanwhile, the XRD result showed that the crystallinity of clinoptilolites remained unchanged after the encapsulation process. The cumulative drug release in the simulated gastric fluid was found to be higher than that in the simulated intestinal fluid, which indicated the potent influence of pH on the release properties of the drugs. The drug release kinetics of metformin HCl from clinoptilolite was best fitted into the Korsmeyer-Peppas model with non-Fickian transport mechanism.Conclusion: We found that clinoptilolite was suitable for DDS application, particularly as a carrier of metformin HCl.

scholarly journals Synthesis of a water-soluble 2,2′-biphen[4]arene and its efficient complexation and sensitive fluorescence enhancement towards palmatine and berberine

2018 ◽  
Vol 14 ◽  
pp. 2236-2241 ◽  
Author(s):  
Xiayang Huang ◽  
Xinghua Zhang ◽  
Tianxin Qian ◽  
Junwei Ma ◽  
Lei Cui ◽  
...  
Keyword(s):  
Association Constant ◽  
Fluorescence Enhancement ◽  
Phosphate Buffer Solution ◽  
Water Soluble ◽  
Binding Affinities ◽  
Buffer Solution ◽  
Solution Ph ◽  
H Nmr ◽  
Naked Eye ◽  
Nmr Signals

A water-soluble 2,2′-biphen[4]arene (2,2’-CBP4) containing eight carboxylato moieties was synthesized and characterized. Its complexation behavior towards two alkaloids, palmatine (P) and berberine (B), was investigated by means of fluorescence and 1H NMR spectroscopy in aqueous phosphate buffer solution (pH 7.4). In the presence of 2,2’-CBP4, 1H NMR signals of P and B displayed very large upfield shifts, indicating the formation of inclusion complexes with strong binding affinities. Fluorescence titration experiments showed that P and B exhibited dramatic fluorescence enhancement of more than 600 times upon complexation with 2,2’-CBP4. Particularly, the fluorescence intensity is strong enough to be readily distinguished by the naked eye. Although the two guests have similar structures, the association constant of B with 2,2’-CBP4 (K a = (2.29 ± 0.27) × 106 M−1) is 3.9 times larger than that of P (K a = (5.87 ± 0.24) × 105 M−1).

scholarly journals Preparation, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Cellulose Aerogel

Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1624
Author(s):  
Lili Qin ◽  
Xinyu Zhao ◽  
Yiwei He ◽  
Hongqiang Wang ◽  
Hanjing Wei ◽  
...  
Keyword(s):  
High Speed ◽  
Drug Carrier ◽  
Phosphate Buffer Solution ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oxidized Cellulose ◽  
Buffer Solution ◽  
Aggregation State ◽  
Cellulose Aerogel

Resveratrol is a natural active ingredient found in plants, which is a polyphenolic compound and has a variety of pharmaceutical uses. Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) was prepared using a freeze-drying method, employing high speed homogenization followed by rapid freezing with liquid nitrogen. RLTAs were designed at varying drug–cellulose aerogel ratios (1:2, 2:3, 3:2, and 2:1). It could be seen via scanning electron microscopy (SEM) that Res integrated into TEMPO-oxidized cellulose (TC) at different ratios, which changed its aggregation state and turned it into a short rod-like structure. Fourier transform infrared (FTIR) spectra confirmed that the RLTAs had the characteristic peaks of TC and Res. In addition, X-ray diffraction (XRD) demonstrated that the grain size of RLTA was obviously smaller than that of pure Res. RLTAs also had excellent stability in both simulated gastric fluid and phosphate buffer solution. The drug release rate was initially completed within 5 h under a loading rate of 30.7 wt%. The results of an MTT assay showed the low toxicity and good biocompatibility of the RLTAs. TC aerogel could be a promising drug carrier that may be widely used in designing and preparing novel biomedicine.

Synthesis, Characterization and In Vitro Drug Release of Melphalan Magnetic Microspheres

2013 ◽  
Vol 22 ◽  
pp. 31-40
Author(s):  
Jin Qiao Xu ◽  
Hai Xing Xu ◽  
Zubad Newaz ◽  
Ran Li ◽  
Yu Zhang ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Drug Release ◽  
Drug Loading ◽  
Phosphate Buffer Solution ◽  
Magnetic Microspheres ◽  
Targeted Chemotherapy ◽  
Buffer Solution ◽  
Magnetization Measurements ◽  
Co Precipitation

A new method of reversible association of melphalan (MEL) to magnetic Fe3O4 nanoparticles preparing MEL magnetic microspheres was developed for magnetically targeted chemotherapy. The efficacy of this approach was evaluated in terms of encapsulation efficiency (EE), drug loading content (DLC), delivery properties and cytotoxicity in vitro. Magnetic Fe3O4 nanoparticles were synthesized by co-precipitation methods and characterized by X-ray diffraction (XRD), fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM) and magnetization measurements. The MEL magnetic microspheres were obtained through emulsion cross-linking method and characterized by FTIR, magnetization measurements and scan electron microscopy (SEM). The EE and DLC were determined using a Spectro Vision DB-18805 spectrophotometer. The MEL magnetic microspheres showed good EE values, between 60.6% and 75.6%, as well as good DLC values, between 16.7% and 32.2%, and the magnetic properties were not significantly affected by incorporation of the drug. The in vitro drug release study was carried out in phosphate buffer solution (PBS), simulating physiologic body fluid conditions at 37o C with pH = 7.4. The release profiles showed an initial fast release rate, which decreased as time progressed; about 60% of the drug was released in the first 4 h, and about 78.23 % had been released after 24 h. The results indicated that the prepared magnetic microspheres may be useful for potential applications of MEL for magnetically targeted chemotherapy.

scholarly journals Azobenzene functionalized mesoporous AlMCM-41-type support for drug release applications

2014 ◽  
Vol 12 (7) ◽  
pp. 788-795 ◽  
Author(s):  
Raul-Augustin Mitran ◽  
Daniela Berger ◽  
Laura Băjenaru ◽  
Silviu Năstase ◽  
Cristian Andronescu ◽  
...  
Keyword(s):  
Drug Release ◽  
Phosphate Buffer Solution ◽  
Fold Increase ◽  
Cytostatic Drug ◽  
Buffer Solution ◽  
Significant Toxicity ◽  
Murine Fibroblast ◽  
Mesoporous Support ◽  
Reduced Toxicity ◽  
Silane Precursor

AbstractA light-responsive material, aminoazobenzene functionalized AlMCM-41, was synthesized and characterized in order to be used as carrier for drug delivery devices. The light-induced hydrophobic-hydrophilic switching effect of azobenzene functionalized aluminosilicate was exploited in the release of irinotecan, a cytostatic drug. To obtain the functionalized mesoporous support, an azobenzene-silane precursor was synthesized by coupling 4-(4′-aminophenylazo) benzoic acid with 3-aminopropyl triethoxysilane and further grafted on AlMCM-41. The azobenzene functionalized mesoporous aluminosilicate exhibited no significant toxicity towards murine fibroblast healthy cells and a reduced toxicity towards murine melanocyte cells. The hybrid materials obtained by loading irinotecan on AlMCM-41 (wt. 35.4%) and aminoazobenzene modified AlMCM-41 (wt. 22%), respectively were characterized by FTIR, small and wide angle XRD, N2 adsorption-desorption isotherms and DSC analyses. A two-fold increase in the drug release rate from azobenzene functionalized aluminosilicate in phosphate buffer solution under UV irradiation was noticed, as compared with dark conditions. Moreover, the azobenzene functionalization of AlMCM-41 significantly increased the irinotecan delivery rate and total cumulative release in comparison with the pristine AlMCM-41 in similar conditions.

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