IN VITROCHARACTERIZATION OF TRAMADOL-HCL-LOADED POLYOXALATE MICROSPHERES DESIGNED FOR CONTROLLED DRUG RELEASE

2015 ◽  
Vol 27 (03) ◽  
pp. 1550022
Author(s):  
Cheon Jung Lee ◽  
Su Young Kim ◽  
Hyun Gu Lee ◽  
Jaewon Yang ◽  
Jin Young Park ◽  
...  
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Controlled Drug Release ◽  
Physicochemical Characteristics ◽  
In Vitro Test ◽  
X Ray Diffraction ◽  
Sustained Drug Release ◽  
Release Formulation ◽  
Preparation Conditions

This study evaluates the properties of Tramadol- HCl -loaded polyoxalate (TH-loaded POX) microspheres prepared by oil-in-oil (O1/O2) emulsion solvent evaporation method, specifically designed for sustained drug release. Morphology and physicochemical characteristics of the as-fabricated were studied by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimeter (DSC) and Fourier transform infrared (FTIR) spectroscopy, while the encapsulation efficiency and release profile of drug (Tramadol- HCl , TH) from POX microspheres were assessed by high-performance liquid chromatography (HPLC). The influence of reaction temperature, stirring speed, initial drug ratio, molecular weight (Mw) and concentration of polyoxalate (POX) on the fabrication of TH-loaded POX microspheres were investigated. Results showed that the characteristics of the microspheres and drug-loaded content can be optimized by adjusting the parameters of preparation conditions. Also, the degradation behavior of TH-loaded POX microspheres was evaluated from in vitro test for 2 weeks. Overall, the results showed that POX microsphere can be one of the promising polymers for controlled injection release formulation with site-specific drug release capabilities.

scholarly journals Glibenclamide-Loaded Polyvinylpyrrolidone (PVP) Nanoparticles and Glibenclamide-Loaded Soluplus® Nanomicelles Intended for Parenteral Administration: Effect of Solvents Mixtures on the Electrosprayed Nanoparticles and In vitro Characterization

2021 ◽  
pp. 241-260
Author(s):  
Maryam Al-Ghezi ◽  
Raghad F. Almilly ◽  
Wedad K. Ali
Keyword(s):  
Drug Release ◽  
Physicochemical Characteristics ◽  
Colloidal Dispersions ◽  
Parenteral Administration ◽  
Solvent Mixtures ◽  
X Ray Diffraction ◽  
Sustained Drug Release ◽  
Drug Molecules ◽  
In Vitro Characterization

Background and Objective: Glibenclamide (GB) is showing promising results in central nervous system (CNS) injuries treatment where intravenous administration of GB could overcome the oral limitations and assure maximum bioavailability. Dry powder of GB nanoparticles reconstituted for parenteral administration was prepared through electrospraying. Methods: The drug was incorporated with two polymers, polyvinylpyrrolidone (PVP) and Soluplus® (SP), at ratios 1:4 and 1:2 (GB/polymer). Different solvent mixtures were used to formulate the particles. Physicochemical characteristics were investigated. Results: The size of the GB-PVP nanoparticle ranged between (409-775) nm with a spherical, disk, fractured and, agglomerated morphology, while those of the GB-SP nanomicelles were of (447-785) nm with mostly irregular morphology, in consequence to the used solvents mixtures. The high encapsulation efficiency ≥ 98% reflects the well dispersed drug molecules within the polymer matrix, further confirmed by X-ray diffraction and infrared spectroscopy. GB-SP colloidal dispersions showed neutral zeta potentials with a cloud point of 36 ˚C, indicating prolonged circulation time and stability after parenteral administration. GB/SP nanomicelles at ratio 1:4 showed a sustained drug release reaching ≥ 94% in 36 hours. Conclusion: The GB-SP nanomicelles with extended drug release and regarding physicochemical properties represent a remarkable drug delivery system for parenteral administration.

Preparation, Characterization and In Vitro Evaluation of IVM Loaded Poly(lactic-Co-Glycolic Acid) (PLGA) Microspheres

2011 ◽  
Vol 311-313 ◽  
pp. 1751-1754
Author(s):  
Gui Yu Li ◽  
Xi Hong Lu ◽  
Xue Hu Li ◽  
Lei Tao ◽  
Jian Ping Liang
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
High Performance ◽  
Glycolic Acid ◽  
Drug Release Profile ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Drug Delivery Carrier ◽  
Drug Sustained Release

Drug was encapsulated in a novel copolymers of poly(lactic-co-glycolic acid) (PLGA) to investigate the sustained-release formulation of drug loaded polymer microspheres delivery system. Used a modified solid-in-oil-in-water (S/O/W) emulsion solvent evaporation method to prepare microspheres, its morphology and particle size distribution were estimated by scanning electron microscopy (SEM), the profile of in vitro drug release were assessed by High performance liquid chromatography (HPLC). Finally, an stable release buffer was utilized to obtain a detailed drug release profile, which was analyzed by HPLC also. Results showed that the microspheres morphology, encapsulation efficiency and the cumulative drug release efficiency were appropriate for veterinary medicine using. The modified preparation method was simple and optimized, PLGA microspheres with excellent controlled-release characteristics may serve as drug delivery carrier and may prolong the drug sustained-release effect.

Development and Characterization of Glipizide Loaded Sustained Release Nanoparticles

2019 ◽  
Vol 9 (3) ◽  
pp. 232-242 ◽  
Author(s):  
Rutuja Deshmukh ◽  
Mrunal Waghulde ◽  
Satyendra Mishra ◽  
Jitendra Naik
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Uptake ◽  
Sustained Drug Release ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Fourier Transformed Infrared Spectroscopy ◽  
Wide Range ◽  
Repeated Dosing

Background: Treating the disease like diabetes is essential due to its wide range of spreading and heredity issues. Glipizide is the commonly used drug for the treatment of diabetes. Glipizide loaded sustained release nanoparticles have been developed to avoid repeated dosing. Objective: The study aimed to develop glipizide-loaded sustained release nanoparticles and characterize them for different studies. Methods: The aim of the present study was to develop glipizide-loaded sustained release nanoparticles using different polymers by the solvent evaporation method. The polymers; Eudragit (RS 100) in combination with Polycaprolactone (PCL) were used to encapsulate glipizide. Optimization of all parameters was performed as per Design Expert software by utilizing a 32 full factorial design. The developed nanoparticles were characterized using Fourier transformed infrared spectroscopy, X-ray diffraction, scanning electron microscopy and in-vitro drug release study. Results: FE-SEM showed that the surface morphology of nanoparticles was smooth and spherical as well as in an oval shape. FTIR shows there is no interaction between polymers and drug. XRD results showed that the crystallinity of pure glipizide reduced from 89.5 to 56.7% when converted into sustained release nanoparticles formulation. Sustained drug release over the period of 12 h was observed due to well encapsulation of glipizide by the polymers. Conclusion: Glipizide loaded nanoparticles were developed with good encapsulation efficiency using a combination of two different biocompatible polymers. The drug release behavior showed that they can be used to develop the sustained release formulation to reduce the side effect caused by over drug uptake as compared to the conventional formulation.

scholarly journals Fabrication of bionanocomposite based on LDH using biopolymer of gum arabic and chitosan-coating for sustained drug-release

2020 ◽  
Vol 85 (9) ◽  
pp. 1223-1235 ◽  
Author(s):  
Milad Abniki ◽  
Ali Moghimi ◽  
Fariborz Azizinejad
Keyword(s):  
Drug Release ◽  
Gum Arabic ◽  
X Ray Diffraction ◽  
Sustained Drug Release ◽  
Experimental Conditions ◽  
X Ray ◽  
Model Drug ◽  
Diffraction Patterns ◽  
New Formulation

The study proposed a new formulation to the sustained delivery of mefenamate anions intercalated into Mg?Al layered double hydroxide (LDH) for oral administration. Different experimental conditions were evaluated to incorporate the mefenamic acid (MEF) and gum arabic (GUM) into LDH structure. The LDH?MEF and LDH?MEF/GUM were covered with chitosan (CHIT). In another experiment, LDH?Cl was used to adsorb mefenamate anions and evaluate the mechanism. The products of LDH were characterized by using different techniques such as FESEM (field emission scanning electron microscopy), XRD (X-ray diffraction), FTIR (Fourier transform infrared) spectroscopy and TGA (thermogravimetric analysis). The X-ray diffraction patterns and FTIR analyses confirmed that the MEF and GUM were successfully intercalated into the interlayer space of LDH. TG analysis verified that the thermal stability of intercalated MEF in the form of bionanocomposite (LDH?MEF/ /GUM/CHIT) was enhanced. Finally, In vitro drug release experiments of bionanocomposite at a pH of 1.2 (acidic medium) and a pH of 7.4 (phosphate buffer medium) showed sustained release profiles with mefenamate anions as an anti-inflammatory model drug.

scholarly journals Cytocompatibility and Dielectric Properties of Sr2+ Substituted Nano-Hydroxyapatite for Triggered Drug Release

2019 ◽  
Vol 1 (1) ◽  
pp. 18-24
Author(s):  
Lakshmanaperumal Sundarabharathi ◽  
Mahendran Chinnaswamy ◽  
Hemalatha Parangusan ◽  
Deepalekshmi Ponnamma ◽  
Mariam Al Ali Al-Maadeed
Keyword(s):  
Dielectric Properties ◽  
Drug Release ◽  
Drug Loading ◽  
Sol Gel ◽  
X Ray Diffraction ◽  
Sustained Drug Release ◽  
Model Drug ◽  
Dielectrical Properties ◽  
Living Tissues

Hydroxyapatite (Ca5(PO4)3OH) is a well-known bioceramics material used in medical applications because of its ability to form direct chemical bonds with living tissues. In this context, we investigate the biocompatibility and dielectric properties of Sr2+-substituted hydroxyapatite nanoparticles were synthesized by sol-gel method. The influence of strontium on the crystal structure, functional group, morphological, electrical properties, and biocompatibility of as-synthesized nano-hydroxyapatite samples was analyzed using X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy and field emission scanning electron microscopy (FE-SEM). Dielectrical properties of the bioactive Sr-HA sample were investigated by a dielectric impedance spectroscopy method. The observed results illustrate the incorporation of Sr2+ ions in the apatite lattice could influence the pure HA properties, by reducing the crystallite size and crystallinity quite consistent with the morphology variation. The ac conductivity (σac) increased with an increasing applied frequency confirmed that prepared HA sample exhibited the universal power law nature. Further, the in vitro drug loading and release studies using doxycycline as a model drug demonstrate that the Sr2+ -HA nanoparticles show high drug adsorption capacity and sustained drug release. Thus, the improved bioceramics system could be a promising candidate for future biomedical applications.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCH OF PLUMBAGIN FOR ANTI-FUNGAL ACTIVITIES

2021 ◽  
Vol 12 (2) ◽  
pp. 23-28
Author(s):  
Aman Sharma ◽  
Abhinav Agarwal
Keyword(s):  
Drug Release ◽  
Sustained Drug Release ◽  
Release Formulation ◽  
In Vitro Drug Release ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Weight Variation ◽  
The Matrix ◽  
Anti Fungal

The objective of the current study is to improve the patient compliance and sustained drug release action by herbal medicine which can be achieved by developing alternative drug delivery system. The matrix type transdermal patches containing plumbagin were prepared by solvent evaporation method with different ratios of polymers (HPMC 50cps, PVP K29-32 and EUDRAGIT RS-100). In these matrix type transdermal patches, the PEG (Polyethylene glycol) was used as plasticizer and DMSO (Dimethyl sulfoxide) used as a penetration enhancer. The formulated patches were evaluated for physicochemical parameters like thickness, weight variation, % moisture content, % moisture uptake, % flatness, folding endurance and drug content. In vitro drug release studies were carried out by using the Franz diffusion cell. The cumulative % of drug released in 10 hours from the six batch formulations were 95.66%, 94.2%, 97.33%, 90.13%, 83.75% and 85.71%, respectively. On the basis of in-vitro drug release, formulation (HE-2) was found to be better than other formulation and these were selected for further evaluation such as anti-fungal activity and stability studies.

Helicid-Loaded Zein Microparticles Prepared Using Electrohydrodynamic Atomization

2012 ◽  
Vol 164 ◽  
pp. 487-491
Author(s):  
Deng Guang Yu ◽  
Xia Wang ◽  
Yao Zu Liao ◽  
Ying Li ◽  
Wei Qian ◽  
...  
Keyword(s):  
Drug Release ◽  
Amorphous State ◽  
In Vitro Dissolution ◽  
Infrared Analysis ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Dissolution Tests ◽  
Electrohydrodynamic Atomization

An electrohydrodynamic atomization (EHDA) process was exploited to prepare helicid-loaded zein microparticles. SEM observations showed that all the particles prepared under varied voltages were round and solid with their sizes gradually decreased from 3.4 ± 1.7 to 1.1 ± 0.5 μm as the applied voltages rose from 6 to 18 kV. Wide-angle X-ray diffraction analyses demonstrated that helicid had been totally converted into an amorphous state in the zein matrix microparticles. Attenuated total reflectance Fourier transform infrared analysis disclosed that the hydrogen bonding presented between helicid and zein molecules. In vitro dissolution tests verified that the microparticles were able to provide a fine sustained drug release profile. The present study provides an easy way to develop novel biomaterials for drug delivery and for providing sustained drug release profiles.

scholarly journals Development of Functionalized Carbon Nano-Onions Reinforced Zein Protein Hydrogel Interfaces for Controlled Drug Release

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 621 ◽  
Author(s):  
Narsimha Mamidi ◽  
Aldo González-Ortiz ◽  
Irasema Lopez Romo ◽  
Enrique V. Barrera
Keyword(s):  
Drug Release ◽  
Colloidal Stability ◽  
Controlled Drug Release ◽  
Acoustic Cavitation ◽  
Drug Transporter ◽  
Ph Responsive ◽  
Sustained Drug Release ◽  
In Vitro Degradation ◽  
Selective Delivery

In the current study, poly 4-mercaptophenyl methacrylate-carbon nano-onions (PMPMA-CNOs = f-CNOs) reinforced natural protein (zein) composites (zein/f-CNOs) are fabricated using the acoustic cavitation technique. The influence of f-CNOs inclusion on the microstructural properties, morphology, mechanical, cytocompatibility, in-vitro degradation, and swelling behavior of the hydrogels are studied. The tensile results showed that zein/f-CNOs hydrogels fabricated by the acoustic cavitation system exhibited good tensile strength (90.18 MPa), compared with the hydrogels fabricated by the traditional method and only microwave radiation method. It reveals the magnitude of physisorption and degree of colloidal stability of f-CNOs within the zein matrix under acoustic cavitation conditions. The swelling behaviors of hydrogels were also tested and improved results were noticed. The cytotoxicity of hydrogels was tested with osteoblast cells. The results showed good cell viability and cell growth. To explore the efficacy of hydrogels as drug transporters, 5-fluorouracil (5-FU) release was measured under gastric and intestinal pH environment. The results showed pH-responsive sustained drug release over 15 days of study, and pH 7.4 showed a more rapid drug release than pH 2.0 and 4.5. Nonetheless, all the results suggest that zein/f-CNOs hydrogel could be a potential pH-responsive drug transporter for a colon-selective delivery system.

scholarly journals Hybrid Systems Based on Talc and Chitosan for Controlled Drug Release

Materials ◽  
2019 ◽  
Vol 12 (21) ◽  
pp. 3634 ◽  
Author(s):  
Luciano C. B. Lima ◽  
Caio C. Coelho ◽  
Fabrícia C. Silva ◽  
Andréia B. Meneguin ◽  
Hernane S. Barud ◽  
...  
Keyword(s):  
Drug Release ◽  
Sol Gel ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Therapeutic Window ◽  
X Ray Diffraction ◽  
Release Capacity ◽  
Model Drug ◽  
Drug Incorporation

Inorganic matrices and biopolymers have been widely used in pharmaceutical fields. They show properties such as biocompatibility, incorporation capacity, and controlled drug release, which can become more attractive if they are combined to form hybrid materials. This work proposes the synthesis of new drug delivery systems (DDS) based on magnesium phyllosilicate (Talc) obtained by the sol–gel route method, the biopolymer chitosan (Ch), and the inorganic-organic hybrid formed between this matrix (Talc + Ch), obtained using glutaraldehyde as a crosslink agent, and to study their incorporation/release capacity of amiloride as a model drug. The systems were characterized by X-ray diffraction (XRD), Therma analysis TG/DTG, and Fourier-transform infrared spectroscopy (FTIR) that supported the DDS’s formation. The hybrid showed a better drug incorporation capacity compared to the precursors, with a loading of 55.74, 49.53, and 4.71 mg g−1 for Talc + Ch, Talc, and Ch, respectively. The release assays were performed on a Hanson Research SR-8 Plus dissolver using apparatus I (basket), set to guarantee the sink conditions. The in vitro release tests showed a prolongation of the release rates of this drug for at least 4 h. This result proposes that the systems implies the slow and gradual release of the active substance, favoring the maintenance of the plasma concentration within a therapeutic window.

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