scholarly journals The Mechanism of Improvement of Film Solubility: Design and Evaluation of Film Forming System with Terbinafine as a Model Drug

2021 ◽  
Author(s):  
Jing Zhang ◽  
bohong lu ◽  
Qiuyan Ma ◽  
Shelke Om ◽  
William Wu ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Topical Administration ◽  
Melting Enthalpy ◽  
Film Forming ◽  
Crystallization Inhibitor ◽  
Model Drug ◽  
In Vitro Performance ◽  
Vitro Release ◽  
Film Solubility

Abstract Purpose: Film forming system (FFS) combines the advantages of patch and gel, it is expected to replace small doses of topical administration in the future. This work targets the design and evaluation of HPC-acrylic FFS with different excipients in appearance, rheology and in vitro properties. Also, the reason of improving the solubility of terbinafine film was illustrated by melting enthalpy thermo analysis.Methods: In this work, we prepared 8 HPC-acrylic FFS samples with different excipients, and characterized the film forming solutions and films in appearance, rheological properties, drug crystallization and in vitro performance. Then used melting enthalpy thermo-analysis to explain the mechanism of improvement of film solubility.Results: According to appearance evaluation, the samples which had a small amount of plasticizer could achieve an uniform surface morphology. The XRD and DSC demonstrated HPC could maintain drug amorphous in films. Based on oscillation frequency sweep, short chain plasticizer tributyl citrate (TBC) leading to strong entanglement and hydrogen bonding among the molecules. In vitro release test showed FP1 had favorable release. And the melting enthalpy thermo-analysis explained why FP1 had favorable release. Conclusions: HPC acted as an effective crystallization inhibitor. TBC could lead stronger intermolecular hydrogen bonds. The poloxamer had favorite miscibility with HPC-acrylic FFS. The combination of MCT and poloxamer with HPC resulted in a high Terbinafine solubility.

scholarly journals Development of a Topical Amphotericin B and Bursera graveolens Essential Oil-Loaded Gel for the Treatment of Dermal Candidiasis

2021 ◽  
Vol 14 (10) ◽  
pp. 1033
Author(s):  
Lupe Carolina Espinoza ◽  
Lilian Sosa ◽  
Paulo C. Granda ◽  
Nuria Bozal ◽  
Natalia Díaz-Garrido ◽  
...  
Keyword(s):  
Essential Oil ◽  
Amphotericin B ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Topical Administration ◽  
In Vivo Models ◽  
Topical Gel ◽  
Cutaneous Candidiasis ◽  
Vitro Release

The higher molecular weight and low solubility of amphotericin B (AmB) hinders its topical administration. The aim of this study was to incorporate Bursera graveolens essential oil into an AmB topical gel (AmB + BGEO gel) in order to promote the diffusion of the drug through the skin in the treatment of cutaneous candidiasis. AmB + BGEO gel formulation was determined using a factorial experiment. Physical and chemical parameters, stability, in vitro release profile and ex vivo permeation in human skin were evaluated. In vitro antimicrobial activity was studied using strains of C. albicans, C. glabrata and C. parapsilosis. The tolerability was evaluated using in vitro and in vivo models. AmB + BGEO gel presented appropriate characteristics for topical administration, including pH of 5.85, pseudoplastic behavior, optimal extensibility, as well as high stability and acceptable tolerability. In vitro release studies showed that the formulation releases the drug following a Boltzmann sigmoidal model. Finally, AmB + BGEO gel exhibited higher amount of drug retained inside the skin and lower Minimum Inhibitory Concentration than a formulation sans essential oil. Therefore, these results suggest that the incorporation of B. graveolens essential oil in the formulation could be used as strategy to promote a local effect in the treatment of cutaneous candidiasis.

scholarly journals Microfluidic Fabrication of Monodisperse Microcapsules for Thermo-Triggered Release of Liposoluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 2200
Author(s):  
Yuanyuan Wang ◽  
Yongyue Li ◽  
Jinghua Gong ◽  
Jinghong Ma
Keyword(s):  
Drug Delivery ◽  
Methacrylic Acid ◽  
Environmental Temperature ◽  
In Vitro Release ◽  
Loading Capacity ◽  
Triggered Release ◽  
Model Drug ◽  
Monodisperse Microcapsules ◽  
Vitro Release

Here, we report a novel thermo-triggered-releasing microcapsule for liposoluble drug delivery. Monodisperse microcapsules with a poly(N-isopropylacrylamide-co-methacrylic acid) hydrogel shell and an oil core were successfully fabricated by a double coaxial microfluidic device. Fluorescent dye Lumogen Red F300 as a model liposoluble drug was dissolved in the oil core with controllable loading capacity. The volume phase transition temperature (VPTT) of the microcapsule was adjusted by copolymerizing with the hydrophilic methacrylic acid. The in vitro release study demonstrates that the shells shrink, leading to the thermo-triggered release of the model drug from the microcapsules at the environmental temperature above the VPTT, while the swollen hydrogel shells can protect the encapsulated drug from leakage and contamination below the VPTT. The proposed microcapsule is a promising liposoluble drug delivery system with controllable loading and smart thermo-triggered release.

scholarly journals Preparation and in vitro release kinetics of nitrendipine-loaded PLLA–PEG–PLLA microparticles by supercritical solution impregnation process

RSC Advances ◽  
2019 ◽  
Vol 9 (28) ◽  
pp. 16167-16175 ◽  
Author(s):  
Shiping Zhan ◽  
Jingchang Wang ◽  
Weijing Wang ◽  
Liyun Cui ◽  
Qicheng Zhao
Keyword(s):  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Impregnation Process ◽  
Supercritical Solution ◽  
Model Drug ◽  
Polymer Microparticles ◽  
Kinetics Of ◽  
Vitro Release

In this work, drug-loaded polymer microparticles were prepared by a supercritical solution impregnation (SSI) process with nitrendipine as the model drug and PLLA–PEG–PLLA as the drug carrier.

scholarly journals Synergistic Effect of Ultrasound and Polyethylene Glycol on the Mechanism of the Controlled Drug Release from Polylactide Matrices

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 880
Author(s):  
Wenting Bao ◽  
Xianlong Zhang ◽  
Hong Wu ◽  
Rong Chen ◽  
Shaoyun Guo
Keyword(s):  
Polyethylene Glycol ◽  
Controlled Release ◽  
Drug Release ◽  
Synergistic Effect ◽  
In Vitro Release ◽  
Structure And Properties ◽  
Melt Extrusion ◽  
Model Drug ◽  
Vitro Release

In this paper, the synergistic effect of ultrasound and polyethylene glycol (PEG) on the controlled release of a water soluble drug from polylactide (PLA) matrices was studied. When ultrasound was used following the hot melt extrusion (HME) of the PLA/model drug release system, the release of the model drug (Methylene Blue (MB)) from the PLA when immersed in phosphate buffered saline (PBS) was affected by the variation of the parameters of ultrasound. It was found that no more than 2% PLA dissolved during the in-vitro release study, and the release of the MB from the PLA was diffusion controlled and fit well with the Higuchi diffusion model. Polyethylene glycol (PEG), which has high hydrophilicity and rapid dissolution speed, was blended with the PLA during the melt extrusion to enhance the release of the MB. The analysis of the structure and properties of the in-vitro release tablets of PLA/PEG/MB indicated that the ultrasound could improve the dispersion of MB in the PLA/PEG blends and it could also change the structure and properties of the PLA/PEG blends. Due to the dissolution of the PEG in PBS, the release of the MB from the PLA/PEG drug carrier was a combination of diffusion and erosion controlled release. Thus a new mechanism combining of diffusion and erosion models and modified kinetics model was proposed to explain the release behavior.

scholarly journals Formulation and Evaluation of Captopril Mouth Dissolving Film

2021 ◽  
pp. 54-60
Author(s):  
V. T. Iswariya ◽  
P. Deepika ◽  
Sowjanya Battu
Keyword(s):  
In Vitro Release ◽  
Methyl Cellulose ◽  
Physical And Mechanical Properties ◽  
Solvent Casting ◽  
Disintegration Time ◽  
Film Forming ◽  
Formulation Factors ◽  
The Impact ◽  
Vitro Release

The goal of this research is to develop captopril mouth dissolving films and evaluate the impact of various formulation factors on the physical and mechanical properties of the films, as well as drug release behaviour. In different grades, hydroxypropyl methyl cellulose (HPMC E15 and K4M) was employed as the film forming polymer. Formulation disintegration times were determined to be in the range of (52 2.5 to 125.6 2.02 s). Formula F2 had the fastest disintegration time in vitro (52 2.5 s) and was determined to be acceptable for film production with ideal physicochemical qualities, faster disintegration, and optimal in vitro release. It may be concluded that the solvent casting approach can be used to make captopril mouth dissolving films with a higher dissolution rate and greater patient compliance.

Antheraea pernyi Silk Fibroin Microspheres Carried Lysozyme

2014 ◽  
Vol 915-916 ◽  
pp. 875-878 ◽  
Author(s):  
Juan Wang ◽  
Gui Jun Li ◽  
Rui Jiang ◽  
Zhu Ping Yin ◽  
Shen Zhou Lu
Keyword(s):  
Silk Fibroin ◽  
Release Kinetics ◽  
In Vitro Release ◽  
X Ray Diffraction ◽  
Antheraea Pernyi ◽  
Encapsulation Rate ◽  
Release Field ◽  
Model Drug ◽  
Vitro Release

A method was developed to prepare the Antheraea Pernyi silk fibroin (ASF) microspheres using lysozyme as a model drug to estimate the application of ASF in drug controlled release field. The structure of ASF microsphere carried drug was characterized by X-ray diffraction and FTIR. The morphology and the influence of the microspheres on the degradation of lysozyme were investigated using scanning electron microscope. The results show that encapsulation rate was increased and drug content was decreased with the addition of lysozyme increasing. In vitro release of lysozyme from the ASF particles we demonstrated that the release kinetics depends on the pH. The pH played important roles in controlling lysozyme release profiles. It also can be seen that the degradation speed of lysozyme ASF microspheres slightly larger than the pure ASF microspheres.

Preparation and In Vitro Drug Release Studies of Arginine Loaded Starch Microspheres

2012 ◽  
Vol 602-604 ◽  
pp. 231-234
Author(s):  
Min Peng Zhu ◽  
Su Hong Li
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Extended Period ◽  
Average Diameter ◽  
Soluble Starch ◽  
Raw Material ◽  
Release Studies ◽  
Model Drug ◽  
Vitro Release

Epichlorohydrin crosslinked starch microspheres (ECMs) were synthesized with soluble starch as a raw material and epichlorohydrin as a crosslinker. The characteristics of ECMs were investigated by Scanning Electron Microscopy (SEM) and Fourier Transform InfraRed spectroscopy (FT-IR).The drug loading and in vitro release properties of ECMs were studied using arginine as a model drug. The results indicate that ECMs have a spherical morphology with average diameter about 7μm. The drug loading studies show that after absorption for 1.5 h, the largest amount of drug (drug loading 31mg/g) is loaded when the quantity ratio of ECMs to arginine is 2. In-vitro release studies indicate that the ECMs are effective in controlled releasing arginine over an extended period of about 25 h.

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