Preparation and Crystal Modification of Ibuprofen-Loaded Solid Lipid Microparticles

Long, Chunxia; Zhang, Lijuan; Qian, Yu

doi:10.1016/s1004-9541(06)60107-9

Cited by 33 publications

(22 citation statements)

References 21 publications

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“…The DSC data of the SLMs showed that the melting peaks as well as the enthalpies depend on the PEG and drug contents of the formulations. The physico-chemical compatibility of the drug and the excipients studied by DSC suggested an absence of drug incompatibility, consistent with similar studies (Jaspart et al, 2005;Long et al, 2006;Eradel et al, 2009;Pilaniya et al, 2011). The results revealed the compatibility of gentamicin and the excipients as well as the stability of the drug in the lipid matrix.…”

Section: Discussionsupporting

confidence: 93%

“…Since drug-loaded SLMs formulations containing highest amount of drug (i.e. 3% w/w gentamicin) especially batch C 3 gave the highest permeation flux and coefficient, it implies that sustained release gentamicin dosage form might be developed with this formulation, consistent with some drug-loaded SLMs formulations (Jaspart et al, 2005;Long et al, 2006;Eradel et al, 2009;Pilaniya et al, 2011). Generally, batches C 1 -C 3 gave greater permeation fluxes and coefficients than corresponding batches B 1 -B 3 and A 1 -A 3 SLMs formulations.…”

Section: Discussionmentioning

confidence: 97%

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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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Section: Discussionsupporting

confidence: 93%

Section: Discussionmentioning

confidence: 97%

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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“…SLMs have the advantages of liposomes (possibility of controlled drug release and drug targeting), in addition to these advantages (use of non organic solvent, non-toxicity of the carrier system, chemical and physical storage stability for both the carrier and the drug, low cost of ingredients, not difficult in preparation and high scale-up potential) [7][8][9] . The most important limitation of SLMs is that drugs to be incorporated into SLMs must be lipophilic enough so as to ensure high-entrapment efficiency 10 and to overcome this problem, solid reversed micellar solution (SRMS)-based carriers have been investigated, and successfully employed to achieve controlled release of a hydrophilic drug, zidovudine 11 .…”

Section: Introductionmentioning

confidence: 99%

Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles

Ogbonna

Kenechukwu

Nwobi

et al. 2014

Pharmaceutical Development and Technology

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Context: Formulation, characterization, in vitro and in vivo evaluation of halofantrine-loaded solid lipid microparticles (SLMs). Objective: The objective of the study was to formulate and evaluate halofantrine-loaded SLMs. Materials and methods: Formulations of halofantrine-loaded SLMs were prepared by hot homogenization and thereafter lyophilized and characterized using particle size, pH stability, loading capacity (LC) and encapsulation efficiency (EE). In vitro release of halofantrine (Hf) from the optimized SLMs was performed in SIF and SGF. In vivo study using Peter's Four day suppressive protocol in mice and the mice thereafter subjected to histological studies in kidney and liver. Results: Results obtained indicated that EE of 76.32% and 61.43% were obtained for the SLMs containing 7% and 3% of Hf respectively. The SLMs loaded with 3% of Hf had the highest yield of 73.33%. Time-dependent pH stability analysis showed little variations in pH ranging from 3.49 ± 0.04 to 4.03 ± 0.05. Discussion: The SLMs showed pH-dependent release profile; in SIF (43.5% of the drug for each of H and H) compared with SGF (13 and 18% for H and H respectively) after 8 h. The optimized SLMs formulation and Halfan® produced a percentage reduction in parasitemia of 72.96% and 85.71% respectively. The histological studies revealed that the SLMs formulations have no harmful effects on the kidney and liver. Conclusion: SLMs formulations might be an alternative for patients with parasitemia as there were no harmful effects on vital organs of the mice.

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“…Solid lipid microparticles (SLM) are micro-scale drug carriers possessing matrix made from fatty acid, glyceride, fatty alcohol, and solid wax with high melting points [3]. They combine many advantages of drug carrier systems.…”

Section: Introductionmentioning

confidence: 99%

Solid lipid microparticles: An approach for improving oral bioavailability of aspirin

Gugu

Chime

Attama

2015

Asian Journal of Pharmaceutical Sciences

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Please cite this article as: Gugu T.H., Chime S.A., Attama A.A., Solid lipid microparticles: an approach for improving oral bioavailability of aspirin, Asian Journal of Pharmaceutical Sciences (2015), http://dx.doi.org/ AbstractThe objectives of the work were to develop a lipid based delivery system for aspirin and to evaluate its physicochemical and the pharmacodynamic properties. Aspirin-loaded solid lipid microparticles (SLMs) were formulated by hot homogenization and analysed for their encapsulation efficiency (EE%), in vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Particle size ranged from 33.10 ± 5.85 to 43.50 ± 7.27 μm for batches A1 to A3 SLMs loaded with 1, 3 and 5 % aspirin and containing Poloxamer 407, while batches B1, B2 and B3 formulated with Soluplus as surfactant had particle size range of 31.10 ± 1.46 to 45.60 ± 2.92 μm. Batches A1 and B1 containing 1% of aspirin had the highest EE of 70 and 72 % respectively. Maximum in vitro release of 95.1 and 93.2 % were obtained at 8 h from batches A1 and B1 respectively. SLMs exhibited about 77.8 % oedema inhibition, while the reference had 66.7 % and ulcer inhibition range of 25 -75 %. Aspirin-loaded SLMs exhibited good properties and could be used orally twice daily for the treatment of inflammation.

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Preparation and Crystal Modification of Ibuprofen-Loaded Solid Lipid Microparticles

Cited by 33 publications

References 21 publications

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

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

Formulation,in vitroandin vivoevaluation of halofantrine-loaded solid lipid microparticles

Solid lipid microparticles: An approach for improving oral bioavailability of aspirin

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