scholarly journals Bioactive Glass Nanoparticles as a New Delivery System for Sustained 5-Fluorouracil Release: Characterization and Evaluation of Drug Release Mechanism

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
Abeer M. El-Kady ◽  
Mohammad M. Farag
Keyword(s):  
Drug Release ◽  
Bioactive Glass ◽  
Surface Area ◽  
Delivery System ◽  
Release Mechanism ◽  
Burst Release ◽  
Drug Release Mechanism ◽  
Diffusion Controlled ◽  
Ft Ir

Bioactive glass nanoparticles were synthesized and tested for the first time as a new delivery system for sustained 5-fluorouracil (5-FU) release. They were characterized by TEM, DTA, TGA, and FT-IR. The porosity % and specific surface area of glass nanoparticles were 85.59% and 378.36 m2/g, respectively. Thein vitrobioactivity evaluation confirmed that bioactive glass disks prepared from these nanoparticles could induce hydroxyapatite layer over their surfaces in simulated body fluid. Thein vitrodrug release experiment indicated that glass nanoparticles could serve as long-term local delivery vehicles for sustained 5-FU release. The release profile of 5-FU showed an initial fast release stage followed by a second stage of slower release. The initial burst release of 5-FU in the first day was about 23% (28.92 mg·L−1) of the total amount of loaded 5-FU, while the final cumulative percentage of the 5-FU released after 32 days was about 45.6% (57.31 mg·L−1) of the total amount of loaded 5-FU. The application of different mathematical models indicated that 5-FU was released by diffusion controlled mechanism and suggested that its release rate was dependent on glass particles dissolution, changes of surface area as well as diameter of glass particles, and concentration of loaded drug.

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

scholarly journals FORMULATION AND EVALUATION OF RAMIPRIL MOUTH DISSOLVING FILMS

2019 ◽  
pp. 124-129
Author(s):  
Jasvanth E ◽  
Teja D ◽  
Mounika B ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Release Mechanism ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Preparation And Evaluation ◽  
Pvp K30

Objective: The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of Ramipril to enhance patient convenience, compliance and to improve bioavailability. Methods: MDFs with 0.5% w/w Ramipril were prepared by a solvent casting method using a wet film applicator. The effects of film formers, wetting/solubilizing, saliva stimulating agents and film modifiers on the physicomechanical and in vitro Ramipril release from MDFs were evaluated. Results: The MDFs prepared were transparent, smooth and showed no re-crystallization upon storage. MDFs casted with hydroxypropyl methylcellulose (HPMC) E3 as film former and polyethylene glycol (PEG-400) as plasticizer showed superior Ramipril release rates and good physicomechanical properties when compared to MDFs with E5 and E15 as film formers. HPMC E3 MDFs with polyvinyl pyrrolidone K30 (PVP K30) and sodium lauryl sulphate (SLS) gave superior drug release properties than MDFs without PVP K30 and SLS. The HPMC E3 MDFs with citric acid (CA) as saliva stimulating and xylitol as soothing agent gave significantly superior in vitro drug release than the MDFs without CA and xylitol. Release kinetics data reveals diffusion as a drug release mechanism. Conclusion: From the obtained results, it can be concluded that the administration of Ramipril as MDF may provide a quick onset of action with enhanced oral bioavailability and therapeutic efficacy.

scholarly journals 5-Fluorouracil Release from Chitosan-Based Matrix.Experimental and Theoretical Aspects

2020 ◽  
Vol 57 (3) ◽  
pp. 180-188
Author(s):  
Roxana Iancu ◽  
Stefan Andrei Irimiciuc ◽  
Maricel Agop ◽  
Mihail Frasila ◽  
Maria-Alexandra Paun ◽  
...  
Keyword(s):  
Drug Release ◽  
Polarized Light ◽  
Crosslinking Density ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Morphological Aspects ◽  
Drug Release Mechanism ◽  
The Matrix

A series of four drug release formulations based on 5-fluorouracil encapsulated into a chitosan-based matrix were prepared by in situ hydrogelation with 3,7-dimethyl-2,6-octadienal. The formulations were investigated from structural and morphological aspects by FTIR spectroscopy, polarized light microscopy and scanning electron microscopy. It was established that 5-fluorouracil was anchored into the matrix as crystals, whose dimension varied as a function of the crosslinking density. The in vitro drug release simulated into a media mimicking the physiological environment revealed a progressive release of the 5-fluorouracil, in close interdependence with the crosslinking density. In the context of Pharmacokinetics behavioral analysis, a new mathematical procedure for describing drug release dynamics in polymer-drug complex system is proposed. Assuming that the dynamics of polymer-drug system�s structural units take place on continuous and nondifferentiable curves (multifractal curves), we show that in a one-dimensional hydrodynamic formalism of multifractal variables the drug release mechanism (Fickian diffusion, non-Fickian diffusion, etc) are given through synchronous dynamics at a differentiable and non-differentiable scale resolutions. Finally, the model is confirmed by the empirical data.

scholarly journals DESIGN AND DEVELOPMENT OF TOPICAL HYDROGEL FORMULATION OF IRBISARTAN

2019 ◽  
pp. 79-83
Author(s):  
ZEESHAN SHAIKH
Keyword(s):  
Angiotensin Ii ◽  
Drug Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Angiotensin Ii Receptor ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir

Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug. Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension. Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan. Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.

Local Delivery System Using Thermosensitive Hydrogel and Drug Loading Microspheres for Cartilage Repairing

2014 ◽  
Vol 898 ◽  
pp. 300-303 ◽  
Author(s):  
Lei Wang ◽  
Gang Wu
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Ring Opening ◽  
Drug Loading ◽  
Local Drug Delivery ◽  
Burst Release ◽  
Transition Diagram ◽  
Thermosensitive Hydrogel ◽  
Local Drug Delivery System

A local drug delivery system constituted by hybrid microsphere/thermosensitive hydrogel was fabricated for Osteoarthritis (OA) therapy in the research. The hydrogel were synthesized by ring-opening copolymerization. Microsphere was fabricated by O/W emulsion and solution evaporation method. The properties of the products were characterized by 1HNMR, FTIR and phase transition diagram. The microsphere/hydrogel was prepared for in vitro drug release research. The results showed microsphere/hydrogel hybrid system can alleviate initial burst release. After 650 hours, only 60 percent of the drugs were released. Kinetics research implied the drug release is controlled by diffusion/erosion mechanism.

In vitro drug release mechanism from lipid nanocapsules (LNC)

2010 ◽  
Vol 390 (2) ◽  
pp. 208-213 ◽  
Author(s):  
Mona M.A. Abdel-Mottaleb ◽  
Dirk Neumann ◽  
Alf Lamprecht
Keyword(s):  
Drug Release ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Lipid Nanocapsules ◽  
Drug Release Mechanism

Preparation and drug release mechanism of CTS-TAX-NP-MSCs drug delivery system

2013 ◽  
Vol 456 (1) ◽  
pp. 186-194 ◽  
Author(s):  
Tian Dai ◽  
Enyun Yang ◽  
Yongjun Sun ◽  
Linan Zhang ◽  
Li Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release Mechanism ◽  
Drug Release Mechanism

scholarly journals Formulation and invitro evaluation of oral extended release microspheres of aceclofenac using various natural polymers

2019 ◽  
Vol 1 (2) ◽  
pp. 58-66
Author(s):  
Syed abid ali ◽  
Syed mujtaba pasha ◽  
Omair sohail ahmed ◽  
Omer wasiq ◽  
Mohammed mukaram ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Oral Route ◽  
Aqueous System ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Drug Release Mechanism ◽  
Microsphere Method

In the present work, bioadhesive microspheres of Aceclofenac using Sodium alginate along with Carbopol 934, Carbopol 971, HPMC K4M as copolymers were formulated to deliver Aceclofenac via oral route. The results of this investigation indicate that ionic cross-linking technique Ionotropic gelation method can be successfully employed to fabricate Aceclofenac microspheres. The technique provides characteristic advantage over conventional microsphere method, which involves an “all-aqueous” system, avoids residual solvents in microspheres. FT-IR spectra of the physical mixture revealed that the drug is compatible with the polymers and copolymers used. Micromeritic studies revealed that the mean particle size of the prepared microspheres was in the size range of 512-903µm and are suitable for bioadhesive microspheres for oral administration. The in-vitro mucoadhesive study demonstrated that microspheres of Aceclofenac using sodium alginate along with Carbopol934 as copolymer adhered to the mucus to a greater extent than the microspheres of Aceclofenac using sodium alginate along with Carbopol 971 and HPMC K4M as copolymers. The invitro drug release decreased with increase in the polymer and copolymer concentration. Analysis of drug release mechanism showed that the drug release from the formulations followed non-Fickian diffusion and the best fit model was found to be Korsmeyer-Peppas. Based on the results of evaluation tests formulation coded T4 was concluded as best formulation.

Etoposide-Loaded Microparticles Prepared with Poly (Hydroxybutyrate-Co-Hydroxyvalerate) and Poly(-Caprolactone) Blends: Formulation, Characterization and in vitro Drug Release

1970 ◽  
Vol 1 (3) ◽  
pp. 251-256
Author(s):  
Patel J. K ◽  
Tank H. M
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Evaporation Process ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Drug Entrapment Efficiency ◽  
Solvent Evaporation Process ◽  
Poly Caprolactone

The purpose of this research was to formulate and systematically evaluate etoposide-loaded microparticles. Etoposide microparticles containing poly(hydroxybutyrate-co-hydroxyvalerate) and poly(-caprolactone) were prepared by an emulsion/solvent evaporation process. Microparticles were discrete, spherical and free flowing. The microparticles showed high % of yeild and drug entrapment efficiency. Etoposide-loaded microparticles demonstrated drug sustained releases (up to 200 hours). The drug release mechanism was dependent on the presence of PCL in the microparticles. The release of etoposide caused an increase in the surface area of the microparticles. A Fickian release was determined for the microparticles prepared exclusively with P(HBHV), while non-Fickian release behaviors were found for the P(HBHV)/PCL microparticles.

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