Analgesic and micromeritic evaluations of SRMS-based oral lipospheres of diclofenac potassium

Chime, Salome Amarachi; Umeyor, Chukwuebuka; Onyishi, V.I.; Onunkwo, GC; Attama, AA

doi:10.4103/0250-474x.117436

Cited by 11 publications

(9 citation statements)

References 17 publications

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“…The Higuchi square root of time dependent model describes drug release as a diffusion process and the Hixson–Crowell cube root law assumes that the release rate is limited by the drug particle dissolution rate . For TM‐MβCD‐IC and TM‐HβCD‐IC, the values of the regression coefficients of the Higuchi model (0.75–0.90) were higher than those of the Hixson–Crowell model (0.59–0.82) indicating that the drug release followed the Higuchi equation and the prime kinetics of release were a diffusion controlled mechanism.…”

Section: Resultsmentioning

confidence: 97%

Preparation and characterization of chitosan based hydrogels containing cyclodextrin inclusion compounds or nanoemulsions of thyme oil

Moradi

Barati

Salehi

et al. 2019

Polymer International

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Hydrogels derived from natural polysaccharides are ideal scaffolds for use in biomedical applications. pH‐sensitive polyvinyl alcohol and chitosan hydrogels containing inclusion compounds of thyme oil (TM) with host methyl‐β‐cyclodextrin (MβCD) and hydroxypropyl‐β‐cyclodextrin (HβCD) and TM nanoemulsion (TM‐nano) were prepared via controlled, biocompatible and low cost freeze–thaw method. The structure of the hydrogels was characterized by Fourier transform IR spectroscopy and optical and scanning electron microscopy. The physicochemical properties of the hydrogels such as gel fraction, swelling ratio and tensile properties were measured. The water vapor transmission rate of the hydrogels indicated that they can maintain a moist environment over the wound bed. Encapsulation and release of antibacterial TM from the hydrogels were determined by UV spectroscopy. In all cases, hydrogels with lower amounts of TM evidenced slower and more controlled release. Different kinetic models were applied for evaluating the drug release mechanism. The antibacterial activity of the samples was studied by counting the number of both Gram‐negative and Gram‐positive bacteria surviving in a broth medium and the results proved the antibacterial activity of all prepared hydrogels. The results of an MTT (3‐(4,5‐dimethylthiazol‐2yl)‐2,5‐diphenyltetrazolium bromide) assay indicated more cell viability of TM‐nano hydrogels in comparison with those of TM‐βCD inclusion compounds. Cell attachment observations also showed great biocompatibility of TM‐nano hydrogels. The prepared hydrogels, especially those containing TM‐nano, might be used as potential wound dressings to improve the wound healing process. © 2019 Society of Chemical Industry

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Section: Resultsmentioning

confidence: 97%

Preparation and characterization of chitosan based hydrogels containing cyclodextrin inclusion compounds or nanoemulsions of thyme oil

Moradi

Barati

Salehi

et al. 2019

Polymer International

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“…The determination of drug loading (or drug incorporation) is an important tool to evaluate a potential drug carrier system. [ 9 10 11 21 ] It is obviously desirable to formulate SLMs with high drug content to decrease the amount of SLMs to be administered. The prerequisite to obtain a sufficient LC is a sufficiently high solubility of the drug in the lipid melt.…”

Section: Resultsmentioning

confidence: 99%

“…For the preparation of the SLMs, the melt-emulsification technique was adopted. [ 9 10 11 12 13 14 ] In each case, the SRMS was melted at 75°C, and the aqueous phase containing PEG 4000 and poloxamer 188 at the same temperature was added to the SRMS with gentle stirring with a magnetic stirrer (SR 1 UM 52188, Remi Equip., India), and the mixture was further dispersed with a mixer (T 25 digital Ultra-Turrax ® ; IKA, Staufen, Germany) at 8000 rpm for 5 min. The SLMs suspension obtained after cooling at room temperature was then lyophilized using a freeze-dryer (Amsco GT3, Germany).…”

Section: Methodsmentioning

confidence: 99%

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Investigation of novel solid lipid microparticles based on homolipids from Bos indicus for the delivery of gentamicin

Kenechukwu

Momoh

Umeyor

et al. 2016

Int J Pharma Investig

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Background:The aim of this study was to formulate solidified reverse micellar solution (SRMS)-based solid lipid microparticles (SLMs) using homolipids from tallow fat (Bos indicus) and evaluate its potential for enhanced delivery of gentamicin.Materials and Methods:SLMs were formulated by melt-emulsification using SRMS (15% w/w Phospholipon® 90G in 35% w/w Bos indicus), polyethylene glycol 4000 (PEG) and gentamicin (1.0, 2.0, 3.0% w/w), and characterized with respect to size, morphology, encapsulation efficiency % and pH-dependent stability. The in vitro release of gentamicin from the SLMs was performed in phosphate buffer (pH 7.4) while bioevaluation was carried out using clinical isolates of Staphylococcus aureus and Escherichia coli.Results:Results showed that the lipid matrix accommodated gentamicin in a concentration-dependent manner, and that stable and spherical SLMs with size range of 18.62 ± 1.24-20.59 ± 1.36 μm and 21.35 ± 1.57-50.62 ± 2.37 μm respectively for unloaded and drug-loaded formulations were obtained. The in vitro drug release studies revealed that SRMS-based SLMs could better be used to control the release of gentamicin than gentamicin injection. Results of sensitivity test revealed that the SLMs time-dependently and capacity-limitedly produced greater inhibition zone diameters (IZDs) than the standards, an indication of improved bioactivity against the test organisms, with greater IZDs against S. aureus than E. coli. Overall, SLMs containing 2% w/w SRMS, 3% w/w gentamicin and PEG 4000 entrapped the highest amount of drug, achieved complete drug release and gave highest IZD against the organisms within 420 min, while plain gentamicin gave the least.Conclusion:This research has shown that SLMs based on Bos indicus and P90G is a potential carrier system for dissolution and bioactivity enhancement of gentamicin.

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“…Unfortunately, the oral delivery route is beset with problems such as gastrointestinal (GI) destruction of labile molecules and low levels of macromolecular absorption (Umeyor et al, 2012a). The development of oral forms of many drugs, however, remains a challenge either on account of their stability or their absorption from the GI tract (GIT) thus leading to sub-therapeutic bioavailability (Nnamani et al, 2010;Chime et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin

Kenechukwu¹,

Momoh²,

Nnamani³

et al. 2014

Drug Delivery

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The purpose of this study was to formulate and evaluate novel PEGylated solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) for improved delivery of gentamicin. Lipid matrix (SRMS) [consisting of 15% w/w Phospholipon® 90G (P90G) in 35% w/w dika wax (Irvingia gabonensis) was formulated and characterized by differential scanning calorimetry (DSC). SLMs were formulated by melt-emulsification using the SRMS, PEG 4000 and gentamicin (1.0, 2.0, 3.0% w/w), and their physicochemical as well as pharmacokinetic parameters determined. In vitro permeation of gentamicin from the SLMs through artificial membrane (0.22 μm pore size) was carried out using Franz's cell and phosphate-buffered saline (PBS, pH 7.4) as acceptor medium, while bioevaluation was performed using clinical isolates of Pseudomonas aeruginosa and Staphylococcus aureus. Stable and irregularly-shaped gentamicin-loaded SLMs of size range 34.49 ± 2.56 to 53.52 ± 3.09 µm were obtained. The SLMs showed sustained drug permeation and exhibited time-dependent and capacity-limited bioactivity. Overall, SLMs containing 2% w/w SRMS, 3% w/w gentamicin and PEG 4000 entrapped the highest amount of drug, gave highest IZD against the test organisms and highest permeation flux (5.239 μg/cm(2).min) and permeation coefficient (1.781 × 10(-6)cm/min) within 420 min, while pure gentamicin gave the least. Preliminary in vivo pharmacokinetic studies also showed an AUC-24 of 1507 µg/h/ml for the optimized formulation, while that of oral drug solution was 678 µg/h/ml. This showed a 2.2-fold increase in the systemic bioavailability of gentamicin from the optimized formulation. PEGylated SRMS-based SLMs prepared with heterolipid from Irvingia gabonensis would likely offer a reliable delivery system for gentamicin.

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Analgesic and micromeritic evaluations of SRMS-based oral lipospheres of diclofenac potassium

Cited by 11 publications

References 17 publications

Preparation and characterization of chitosan based hydrogels containing cyclodextrin inclusion compounds or nanoemulsions of thyme oil

Preparation and characterization of chitosan based hydrogels containing cyclodextrin inclusion compounds or nanoemulsions of thyme oil

Investigation of novel solid lipid microparticles based on homolipids from Bos indicus for the delivery of gentamicin

Solid lipid micro-dispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): a novel carrier system for gentamicin

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