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result(s) for
"Emulsion solvent diffusion"
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Biodegradable PLGA Microsphere Formation Mechanisms in Electrosprayed Liquid Droplets
by
Sasai, Aiko
,
Tsujimoto, Hiroyuki
,
Wakisaka, Akihiro
in
electrospray
,
emulsion solvent diffusion method
,
nanosphere
2022
Microspheres composed of poly (lactic-co-glycolic acid) (PLGA) were formed in liquid droplets using the electrospray technique. The structure of the microspheres was controlled by changing the electric voltage of the electrospray. PLGA microspheres with porous structures and micro-sized nanocomposite particles comprising PLGA nanosphere aggregates were formed at 5.0–7.0kV and 2.5–3.5kV, respectively. The structural change was related to the extent of evaporation of the solvent from the droplets during their flight. When the evaporation was completed in the relatively small droplets, the microspheres with porous structures were formed in the droplets. To study the mechanism, we observed the effects of the electric voltage of the electrospray, PLGA concentration, flight distance of the droplets, and molecular weight of PLGA on the structure of the PLGA particles. The novelty of this study is the analysis of the size and structure of the PLGA microparticles, which were controlled by the electrospray technique. Therefore, this research has important implications for the structural design and preparation of nanocomposite particles.
Journal Article
Development and Characterization of Polymeric Idebenone Spherical Agglomerates by Quasi-emulsion Solvent Diffusion Technique
by
Detholia, Krunal K.
,
Mohandas, Amrutha A
,
Jadeja, Mukesh B.
in
Bioavailability
,
Chromatography
,
Drug dosages
2025
Idebenone spherical agglomerates were prepared to improve micromeritics properties and solubility. The polymeric spherical agglomerates of Idebenone were developed by Quasi-emulsion solvent diffusion technique comprising three different solvents, methanol (good solvent), dichloromethane (bridging liquid) and water (poor solvent). A Pseudo ternary phase diagram was utilized to select and optimize the solvent system. The hydrophilic polymer PVP K30 was used as a medium stabilizer. The spherical agglomerates underwent a series of physicochemical assessments, including measurements of the angle of repose, Carr's index, Hausner's ratio, % yield, and shape. The optimized formulation exhibited a favourable angle of repose of 29.4°±0.034, and the % drug release after 30 minutes reached 83.11±3.8, surpassing all other concentrations. The optimized batch was further subjected to thorough analysis, encompassing Gas Chromatography to detect residual solvent levels and SEM, FT-IR, XRPD, drug content, and in-vitro dissolution studies. Subsequently, fast dispersible tablets were prepared using the optimized batch. For assessing stability, the optimized formulation underwent accelerated stability studies over a month at 40±2°C / 75±5% RH. These tests revealed negligible alterations in flowability, drug content, % yield, and drug release profile. The findings suggest that the polymeric spherical crystal agglomerates improve the micrometric properties and solubility of Idebenone.
Journal Article
Microsponges: a promising frontier for prolonged release-current perspectives and patents
by
Vishwanath, B. A.
,
Srinatha, N.
,
Battu, Sowjanya
in
Active control
,
Biopharmaceuticals
,
Controlled release
2024
Background
Microsponges are one of the advanced drug delivery systems that facilitates precise and controlled release of active ingredients that are suitable for topical and oral use. These porous microspheres are typically sized between 5 and 300 μm, offer benefits including controlled release, stability, and minimized side effects. Manufacturing techniques like quasi-emulsion solvent diffusion and liquid–liquid suspension polymerization are usually employed to prepare microsponges, although various challenges arise from the use of potentially hazardous organic solvents.
Main body
Microsponges possess distinct traits such as extended drug release, formulation flexibility, and high drug loading capacity. Entrapment of drugs requires considerations of solubility, stability, and miscibility, while evaluation methods encompass production yield and particle size analysis. Their applications range from dermatological to biopharmaceutical delivery, with diverse products utilizing this technology. Ongoing innovations about microsponges are evident in patents concerning medical dressings and hyaluronic acid delivery systems.
Conclusion
Microsponges present a promising avenue in drug delivery, despite many challenges. Current review addresses on limitations and diverse products highlighting commercial viability. Patent activity signifies continued interest, suggesting significant potential for enhancing patient care.
Journal Article
In vitro characterization and in vivo antidiabetic studies of designed formulations: nanosponges and nanocrystals of voglibose
by
Guleria, Rajender
,
Dahiya, Dev Prakash
,
Aneja, Preeti
in
Antidiabetics
,
Bioavailability
,
Box–Behnken design
2025
Background
Diabetes mellitus is the main root of mortality worldwide and a major cause of death by 2030. As the global medical landscape shifts, diabetes presents a serious challenge to standard treatment methods. Orally administered insulin, used for treatment, has drawbacks including instability in the gastrointestinal system due to degrading enzymes and low absorption, resulting in comparatively poor uptake. Nanotechnology introduces remarkable possibilities for diabetes treatment through targeted and accurate drug delivery. Among various nanodosage forms, nanosponges and nanocrystals are considered the most appropriate strategy for diabetes care. The study intends to enhance the bioavailability of voglibose by encapsulating it in a voglibose nanosponges formulation (V-NSF) and a voglibose nanocrystals formulation (V-NCF). Design of experimentation was successfully carried out using the Box–Behnken design. The response parameters, essentially particle size, entrapment efficiency and PDI, have been speculated, followed by observed values using a particle size analyzer and entrapment efficiency methods. Various characterization parameters, such as in vitro drug release, FTIR, thermal analysis (DSC and XRD) and surface morphology (SEM), were used to analyze the results, accompanied by stability studies of the optimized formulation and in vivo studies performed using Sprague–Dawley rats.
Results
The particle size of V-NSF was 270.63 ± 5.9 nm, and the PDI value was 0.165 ± 0.027. Entrapment efficiency was 78 ± 0.32%. In case of V-NCF, particle size was analyzed as 131 ± 0.31 nm, PDI value of NCF was 0.140 ± 0.006, and entrapment efficiency was 74 ± 0.28%. All physical and chemical characterization parameters were confirmed by FTIR, SEM, DSC, XRD and in vitro release.
Conclusion
V-NSF and V-NCF exhibited confined size distribution, acceptable polydispersity index and greater value of entrapment efficiency. The pharmacodynamic studies showed that V-NSF elicits a remarkable antidiabetic effect compared to V-NCF, with moderate efficacy than voglibose itself. The data of optimized formulations can be useful for clinical implications and suggest that V-NSF and V-NCF could be effective in diabetic management.
Graphical abstract
Journal Article
Biodegradable PLGA Microsphere Formation Mechanisms in Electrosprayed Liquid Droplets
by
Sasai, Aiko
,
Tsujimoto, Hiroyuki
,
Wakisaka, Akihiro
in
Aqueous solutions
,
Biodegradability
,
Droplets
2022
Microspheres composed of poly (lactic-co-glycolic acid) (PLGA) were formed in liquid droplets using the electrospray technique. The structure of the microspheres was controlled by changing the electric voltage of the electrospray. PLGA microspheres with porous structures and micro-sized nanocomposite particles comprising PLGA nanosphere aggregates were formed at 5.0–7.0 kV and 2.5–3.5 kV, respectively. The structural change was related to the extent of evaporation of the solvent from the droplets during their flight. When the evaporation was completed in the relatively small droplets, the microspheres with porous structures were formed in the droplets. To study the mechanism, we observed the effects of the electric voltage of the electrospray, PLGA concentration, flight distance of the droplets, and molecular weight of PLGA on the structure of the PLGA particles. The novelty of this study is the analysis of the size and structure of the PLGA microparticles, which were controlled by the electrospray technique. Therefore, this research has important implications for the structural design and preparation of nanocomposite particles.
Journal Article
Agglomeration of Celecoxib by Quasi Emulsion Solvent Diffusion Method: Effect of Stabilizer
by
Nokhodchi, Ali
,
Maghsoodi, Maryam
in
Celecoxib
,
Quasi emulsion solvent diffusion method
,
Spherical crystallization
2016
Purpose: The quasi-emulsion solvent diffusion (QESD) has evolved into an effective technique to manufacture agglomerates of API crystals. Although, the proposed technique showed benefits, such as cost effectiveness, that is considerably sensitive to the choice of a stabilizer, which agonizes from a absence of systemic understanding in this field. In the present study, the combination of different solvents and stabilizers were compared to investigate any connections between the solvents and stabilizers. Methods: Agglomerates of celecoxib were prepared by QESD method using four different stabilizers (Tween 80, HPMC, PVP and SLS) and three different solvents (methyl acetate, ethyl acetate and isopropyl acetate). The solid state of obtained particles was investigated by differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopy. The agglomerated were also evaluated in term of production yield, distribution of particles and dissolution behavior. Results: The results showed that the effectiveness of stabilizer in terms of particle size and particle size distribution is specific to each solvent candidate. A stabilizer with a lower HLB value is preferred which actually increased its effectiveness with the solvent candidates with higher lipophilicity. HPMC appeared to be the most versatile stabilizer because it showed a better stabilizing effect compared to other stabilizers in all solvents used. Conclusion: This study demonstrated that the efficiency of stabilizers in forming the celecoxib agglomerates by QESD was influenced by the HLB of the stabilizer and lipophilicity of the solvents.
Journal Article
A review on nanosponges-A promising novel drug delivery system
by
Abdelmagid, Khilifa Fathelrahman Khalifa
,
Nitish
,
Jeganath, S.
in
Cellulose
,
Chromatography
,
Drug delivery systems
2021
The dispersed product comprising ethyl cellulose and drug was diluted in 20ml dichloromethane and gradually applied in 150ml of aqueous persistent solution to a certain volume of polyvinyl alcohol The solution of the process was stirring for 2 hours at 1000 rpm. Type of drugs[19]: Drug molecules ought to have those attributes described below in order to be complexed with nanosponges. 1) The drug's molecular weight must be between 100 and 400 Daltons. 2) There are less than five compact rings in the drug molecule. 3) Water solubility should be below 10mg/ml. Microscopy studies[21]: Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) could be used to study the drug, nanosponges and product microscopic features (drug / nanosponge complex). Fourier Transform Infrared (FTIR) Analysis: In order to ascertain the potential for interference of chemical bonds between drug and polymer, Fourier transform infrared analysis was performed.
Journal Article
Formulation and in vitro evaluation of metformin hydrochloride loaded microspheres prepared with polysaccharide extracted from natural sources
by
Kanta Nath, Lila
,
Lahkar, Sunita
,
Sharma, Hemanta Kumar
in
Abelmoschus - chemistry
,
Abelmoschus esculentus
,
Bora rice
2013
The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study
Journal Article
Formulation and Evaluation of Amisulpride Nanocrystal Tablets
by
Sathali, Abdul Hasan A
,
Prakash, Jeya Chandra S.K
in
Amisulpride
,
Emulsion Solvent Diffusion
,
High Pressure Homogenization
2015
Amisulpride is an antipsychotic drug which belongs to BCS type II classification. The present study aims to develop nanocrystals of amisulpride in order to enhance solubility and dissolution rate by decreasing particle size of drug. The amisulpride nanocrystals with small and uniform particle size were successfully prepared by emulsion solvent diffusion method is based on the high pressure homogenization technique using βcyclodextrin, sodium lauryl sulphate, hydroxy propyl methyl cellulose E15 and polyvinyl alcohol as stabilizers at different concentrations. The compatability studies was done by infrared spectroscopy and differential scanning calorimetry showed that no interaction between the drug and stabilizers. The amisulpride nanocrystals were evaluated for drug content, invitro dissolution study, SEM, X-ray powder diffraction, particle size distribution, zeta potential and solubility studies. The X-ray powder diffraction (XRPD) confirmed that there was no change in the crystalline state by this size reduction process. The presence of stabilizers made the nanocrystal formulations more stable. The solubility and in vitro dissolution studies suggested that the nanocrystal formulations can improve the bioavailability of the amisulpride by improving its solubility and dissolution rate when compared to pure drug. It was showed that BCD 1.8% concentration gives better drug release profile and enhances the solubility. The amisulpride nanocrystal tablets were successfully prepared from the best formulation by direct compression method. Precompression and post compression evaluation studies are also performed. Amisulpride nanocrystal tablet showed better drug release profile when compared to marketed and amisulpride tablet.
Journal Article