scholarly journals Ibuprofen-Loaded Chitosan–Lipid Nanoconjugate Hydrogel with Gum Arabic: Green Synthesis, Characterisation, In Vitro Kinetics Mechanistic Release Study and PGE2 Production Test

Gels ◽  
2021 ◽  
Vol 7 (4) ◽  
pp. 254
Author(s):  
Syed Mahmood ◽  
Samah Hamed Almurisi ◽  
Khater AL-Japairai ◽  
Ayah Rebhi Hilles ◽  
Walla Alelwani ◽  
...  
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Gum Arabic ◽  
Pge2 Production ◽  
Production Test ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Transdermal Administration ◽  
In Vitro Drug Release

Ibuprofen is a well-known non-steroidal anti-inflammatory (NSAID) medicine that is often used to treat inflammation in general. When given orally, it produces gastrointestinal issues which lead to lower patient compliance. Ibuprofen transdermal administration improves both patient compliance and the efficacy of the drug. Nanoconjugation hydrogels were proposed as a controlled transdermal delivery tool for ibuprofen. Six formulations were prepared using different compositions including chitosan, lipids, gum arabic, and polyvinyl alcohol, through ionic interaction, maturation, and freeze–thaw methods. The formulations were characterised by size, drug conjugation efficiency, differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). Further analysis of optimised hydrogels was performed, including X-ray diffraction (XRD), rheology, gel fraction and swelling ability, in vitro drug release, and in vitro macrophage prostaglandin E2 (PGE2) production testing. The effects of ibuprofen’s electrostatic interaction with a lipid or polymer on the physicochemical and dissolution characterisation of ibuprofen hydrogels were evaluated. The results showed that the S3 (with lipid conjugation) hydrogel provided higher conjugation efficiency and prolonged drug release compared with the S6 hydrogel.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Swelling Behaviour ◽  
X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

scholarly journals Characterization of bilayered matrix-type mucoadhesive buccal films containing tizanidine hydrochloride and piroxicam

2021 ◽  
Vol 20 (11) ◽  
pp. 2241-2248
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Residence Time ◽  
Ex Vivo ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Folding Endurance ◽  
Buccal Films

Purpose: To formulate and characterize tizanidine hydrochloride (TZN) and piroxicam (PRX)-loaded bilayer mucoadhesive buccal films with an intention to improve the bioavailability and patient compliance in pain management.Methods: Bilayer buccal films were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC) 15cps and polyvinylpyrrolidone (PVP K30 as immediate release (IR) layer forming polymers and HPMC K15 M, PVP K 90 along with various muco adhesive polymers (Carbopol P934, sodium alginate, etc), as sustained release (SR) layer forming polymers. The prepared films werecharacterized for thickness, weight variation, folding endurance, surface pH, swelling index,mucoadhesive strength, in vitro residence time, in vitro drug release, ex vivo permeation and drug release kinetics.Results: The prepared films were of largely uniform thickness, weight and drug content. Moisture loss (%) and folding endurance were satisfactory. Surface pH was compatible with salivary fluid. Disintegration time was 85 s for F1 and 115 s for F2 of IR films. In vitro dissolution studies showed 99.12 ± 1.2 % (F1) and 90.36 ± 1.8 % (F2) were released in 45 min. Based on the above results, F1 was chosen as the optimum formulation to be combined with SR layer of TZN. Amongst the SR layers of TZN in vitro drug release. The findings show that of F2 was 98.38 ± 0.82 % and correlated with ex vivo release. Drug release followed zero order release kinetics and mechanism of drug release was non-Fickian type diffusion. In vitro residence time was greater than 5 h.Conclusion: The findings show that the bilayer buccal films demonstrate the dual impact of deliveringPRX instantly from the IR layer, with good controlled release and permeation of TZN from the SR layer, thus providing enhanced therapeutic efficacy, drug bioavailability and patient compliance.

pH-Sensitive Interpenetrating Hydrogel for Eradication of Helicobacter pylori

2010 ◽  
Vol 3 (2) ◽  
pp. 924-932
Author(s):  
A K Gupta ◽  
Maurya S D ◽  
R C Dhakar ◽  
R D Singh
Keyword(s):  
Drug Release ◽  
Ph Value ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Crosslinking Process ◽  
Drug Entrapment Efficiency ◽  
Crosslinking Agents ◽  
Polymer Ratio

The interpenetrating hydrogels of clarithromycin were prepared by chemical crosslinking process using chitosan, poly (vinylpyrrolidone) and poly (acrylic acid) polymers and glutaraldehyde and N,N’-methylenebisacrylamide as crosslinking agents. The hydrogels were evaluated for FTIR analysis, differential scanning calorimetry (DSC), drug entrapment efficiency, scanning electron microscopy (SEM), swelling study, in-vitro drug release and mucoadhesive study. The formulation containing higher amount of chitosan showed greater swelling and drug release because of higher amount of NH2 as pendant group, which ionize at lower PH values. Finally, it was concluded that by appropriate modification of polymer ratio the extent of swelling and rate of drug release can be modulated. The result showed that IPN hydrogels prepared release the drug at lower PH value (PH 2.0) or in stomach thus maintaining antibiotic concentration in stomach for prolonged period of time.

Hydrodynamically Balanced Capsule of Famotidine: An Improved Delivery via Gastroretentive Hydrogels

2021 ◽  
pp. 4573-4579
Author(s):  
Ritesh Kumar ◽  
Kashmira J. Gohil
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Release Kinetics ◽  
Mixing Time ◽  
Fickian Diffusion ◽  
Absolute Bioavailability ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release

Objective: The aim of the present study was to increase the absolute bioavailability of famotidine, enhanced patient compliance in the treatment of peptic ulcer by increasing its gastric residence time and controlled local release of drug upto 12 hours. Materials and Methods: Hydrodynamically balanced capsules of famotidine were prepared, consisting of floating matrix granules, which formed hydrogels. Effects of different formulation variables namely hypromellose (HPMC 4000 cps, HPMC 5600 cps, HPMC 15000 cps), effervescent agent (potassium bicarbonate) and mixing time were studied. Optimization study included 23 full factorial design with t50% and t80% as the kinetic parameters (response variable). Matrix characterization included scanning electron microscopy. All prepared formulations were evaluated to various parameters such as micromeritics properties, % buoyancy and in vitro drug release studies. Results and Discussion: The optimized formulation (F4) remains buoyant for more than 12 hrs. The in-vitro drug release study indicated that increasing the viscosity of HPMC resulted in sustained drug release with long floating duration. SEM studies showed definite entrapment of the drug in the matrix and hydrogel formation. Results showed a pH independent but polymer viscosity dependent drug release profile. The release kinetics followed Higuchi model and mechanism of release was found to be non-Fickian diffusion. Conclusion: Famotidine-loaded hydrodynamically balanced capsules were successfully prepared and prove to be useful for prolonged gastric residence of the drug, better bioavailability, patient compliance and improve delivery for enhanced anti-ulcer activity.

Beta-Cyclodextrin and Maltodextrin Based Solid Dispersion of Meloxicam to Enhance the Solubility of Meloxicam; Formulation and In-vitro Evaluation

2019 ◽  
Vol 41 (1) ◽  
pp. 133-133
Author(s):  
Muhammad Zaman Muhammad Zaman ◽  
Muhammad Hanif Muhammad Hanif ◽  
Syed Saeed Ul Hassan Syed Saeed Ul Hassan ◽  
Javed Iqbal and Muhammad Ahmad Shehzad Javed Iqbal and Muhammad Ahmad Shehzad
Keyword(s):  
Solid Dispersion ◽  
X Ray Diffraction ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
X Ray ◽  
Beta Cyclodextrin ◽  
Release Studies ◽  
Pure Drug

The purpose of the current study was to enhance the solubility of the meloxicam (MLX) by preparing complex with β-Cyclodextrin (CD) and maltodextrin (MD). Dextrins have the ability to capture the drug inside their cavities without forming any chemical bonding. Three (3) formulations, each of solid dispersion (SD) and physical mixture (PM) were prepared by using different drug to polymer ratios (1:4, 1:6 and 1:8) followed by evaluation for micromeritic properties, drug contents, and in vitro drug release studies, scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and x-ray diffraction (XRD) studies. Chemical compatibility of the ingredients was evaluated by using Fourier transform infrared spectroscopy (FTIR). Results of conducted studies exposed excellent flow properties of SDs as well as prepared PMs, with reasonable amount of loaded drug, i.e. andgt;90%. SEM showed a bit irregular surface while XRD suggested crystalline behavior of pure drug, which was masked after its conversion into SDs and PMs based on dextrins. Solubility of the MLX was increased significantly form its initial extent of solubility i.e. 12.5 and#181;g/ml in pure form to 786.72 and#181;g/ml in the form of SD (pandlt;0.05), advocating suitability of materials and methods for solubility enhancement of MLX.

scholarly journals Encapsulation of Diclofenac Molecules into Poly(-Caprolactone) Electrospun Fibers for Delivery Protection

2009 ◽  
Vol 2009 ◽  
pp. 1-8 ◽  
Author(s):  
Loredana Tammaro ◽  
Giuseppina Russo ◽  
Vittoria Vittoria
Keyword(s):  
Diclofenac Sodium ◽  
Composite Fibers ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Electrospinning Technique ◽  
In Vitro Drug Release ◽  
Good Thermal Stability ◽  
Fibrous Membranes ◽  
Poly Caprolactone

Mg-Al Hydrotalcite-like clay (LDH) intercalated with diclofenac anions (HTlc-DIC) was introduced into poly(-caprolactone) (PCL) in different concentrations by the electrospinning technique, and mats of nonwoven fibers were obtained and compared to the pristine pure electrospun PCL. The fibers, characterized by X-ray diffraction, thermogravimetric analysis, and differential scanning calorimetry, show an exfoliated clay structure up to 3 wt%, a good thermal stability of the diclofenac molecules and a crystallinity of PCL comparable to the pure polymer. The scanning electron microscopy revealed electrospun PCL and PCL composite fibers diameters ranging between 500 nm to 3.0 m and a generally uniform thickness along the fibers. As the results suggested the in vitro drug release from the composite fibers is remarkably slower than the release from the corresponding control spun solutions of PCL and diclofenac sodium salt. Thus, HTlc-DIC/PCL fibrous membranes can be used as an antinflammatory scaffold for tissue engineering.

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.

Preparation of ciprofloxacin-encapsulated poly-ε- caprolactone microcapsules by the solvent evaporation technique

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Marta Przybyslawska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
Evaporation Technique

Abstract The objective of this study was to prepare ciprofloxacin (CIP) encapsulated poly-ε-caprolactone (PCL) microcapsules by the single emulsion oilin- water (o/w) solvent evaporation method. The obtained microcapsules were characterized for size, morphology, drug loading and entrapment efficiency. The physical state of microcapsules was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). Storage stability, the in vitro drug release and mathematical modeling of drug release were also tested. It was found that obtained microcapsules had spherical shape and their size range was from 57.5 μm to 234.7 μm. The drug loading of microcapsules was from 1.72% to 11.02%. The optimal conditions of the encapsulation process include the drug/polymer ratio 2/1, using homogenizer for 5 min at 15000 rpm to disperse CIP in PCL solution and aqueous phase at pH 5.5. The results of CIP release study indicate that obtained microcapsules might be successfully used for designing sustained release dosage forms.

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