Molecular interaction between glimepiride and Soluplus ® -PEG 4000 hybrid based solid dispersions: Characterisation and anti-diabetic studies

Reginald-Opara, Joy N.; Attama, Anthony A.; Ofokansi, KC; Umeyor, Chukwuebuka; Kenechukwu, Franklin Chimaobi

doi:10.1016/j.ijpharm.2015.11.007

Cited by 41 publications

(24 citation statements)

References 25 publications

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“…The slow dissolution rate and low solubility of some drugs lead to unpredictable bioavailability, non-reproducible clinical response or treatment inefficiency due to low therapeutic plasma levels; therefore, their use must be optimized using formulation strategies capable of improving their administration [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

et al. 2020

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This review aims to provide an overview of studies that address the use, in therapeutic applications, of solid dispersions (SDs) with biological activities in vitro and/or in vivo mainly made up of polymeric matrices, as well as to evaluate the bioactive activity of their constituents. This bibliographic survey shows that the development of solid dispersions provides benefits in the physicochemical properties of bioactive compounds, which lead to an increase in their biological potential. However, despite the reports found on solid dispersions, there is still a need for biological assay-based studies, mainly in vivo, to assist in the investigation and to devise new applications. Therefore, studies based on such an approach are of great importance to enhance and extend the use of solid dispersions in the most diverse therapeutic applications.

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Section: Introductionmentioning

confidence: 99%

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

et al. 2020

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“…The use of PEG to enhance solubilization has severally been reported [ 32 , 36 , 37 ]. The strong fungicidal efficacy of the SLMs containing MN could also be related to improved solubilization conferred on the drug by the surfactant properties of Soluplus® and Tween® 80 as well as the membrane penetration-enhancing property of PEG 4000 [ 38 , 41 , 50 ].…”

Section: Resultsmentioning

confidence: 99%

“…In addition, time-kill assays also confirmed that MN-loaded PEGylated SLMs had stronger fungicidal activity than their non-PEGylated counterparts. The observed fast-acting and strong fungicidal activity of MN-loaded SLMs could be related to improved lipid solubility conferred on the drugs by the surfactant properties of Soluplus® and Tween® 80, which ensured sustained delivery of the drugs through gradual and sustained erosion of the lipid matrix coupled with the penetration-enhancing property of PEG 4000 [ 36 , 37 , 41 , 50 ]. The developed formulation could be useful alternative to Fungusol® topical lotion in the treatment of fungal infections caused by MN-susceptible microorganisms such as C. albicans (implicated in VVC).…”

Section: Resultsmentioning

confidence: 99%

Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate

Kenechukwu

Attama

Ibezim

et al. 2018

BioMed Research International

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The aim of this study was to investigate the potential of microparticles based on biocompatible phytolipids [Softisan® 154 (SF) (hydrogenated palm oil) and super-refined sunseed oil (SO)] and polyethylene glycol- (PEG-) 4000 to improve intravaginal delivery of miconazole nitrate (MN) for effective treatment of vulvovaginal candidiasis (VVC). Lipid matrices (LMs) consisting of rational blends of SF and SO with or without PEG-4000 were prepared by fusion and characterized and employed to formulate MN-loaded solid lipid microparticles (SLMs) by melt-homogenization. The SLMs were characterized for physicochemical properties, anticandidal activity, and stability. Spherical discrete microparticles with good physicochemical properties and mean diameters suitable for vaginal drug delivery were obtained. Formulations based on SO:SF (1:9) and containing highest concentrations of PEG-4000 (4 %w/w) and MN (3.0 %w/w) were stable and gave highest encapsulation efficiency (83.05–87.75%) and inhibition zone diameter (25.87±0.94–26.33±0.94 mm) and significantly (p<0.05) faster and more powerful fungicidal activity regarding killing rate constant values (7.10 x 10−3–1.09 x 10−2 min−1) than commercial topical solution of MN (Fungusol®) (8.00 x 10−3 min−1) and pure MN sample (5.160 x 10−3 min−1). This study has shown that MN-loaded SLMs based on molecularly PEGylated lipid matrices could provide a better option to deal with VVC.

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“…DSC is a measurement tool that gives insight into the thermal properties of ingredients and formulations in terms of melting point, enthalpy and glass transition temperature 18,21,51 . Summarily, high enthalpy values suggest high crystallinity of systems and vice versa.…”

Section: Discussionmentioning

confidence: 99%

In vivo antiplasmodial potential of Carrageenan and Prosopis africana buccal films of artemether on malariogenic mice

Nnamani

Nnadi

Ibezim

et al. 2020

J. Drug Delivery Ther.

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Objective: To deliver bioadhesive buccal films of artemether (ART) with ability to adhere, hydrate and release drug across the buccal membrane. Methods: Buccal films prepared by film casting using carrageenan (CAR) and Prosopis africana (PRO) were characterized by size, zeta potential, texture, water content, morphology, thermal and interaction studies, in vitro and in vivo antiplasmodial activity in mice. Results: Films were stable with sizes (2442 and 835 nm), water content (21 and 15 %), bioadhesivity (24 and 9.4 %) and film thickness (0.18 and 0.28 mm) for CARART and PROART respectively. Enthalpy of CARART, PROART and ART were 76, 22 and 88 J/g where as parasitaemia reduction of 67 and 76 % were observed for CARART and PROART respectively. Conclusion: Though CARART had better water content and bioadhesivity necessary for film hydration at buccal membrane, PROART eventually had superior buccal performance perhaps due to its film thickness and amorphous nanoparticle subdivision. Key words: Artemether; Carrageenan; Prosopis africana; Sublingual buccal films; Malaria

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Molecular interaction between glimepiride and Soluplus ® -PEG 4000 hybrid based solid dispersions: Characterisation and anti-diabetic studies

Cited by 41 publications

References 25 publications

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate

In vivo antiplasmodial potential of Carrageenan and Prosopis africana buccal films of artemether on malariogenic mice

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