&lt;i&gt;In vitro&lt;/i&gt; and &lt;i&gt;In vivo&lt;/i&gt; Characterisation of Piroxicam-Loaded Dika Wax Lipospheres

Brown, S A; Chime, Salome Amarachi; Attama, Anthony A.; Agu, Confidence I; Onunkwo, Godswill C.

doi:10.4314/tjpr.v12i1.6

Cited by 7 publications

(8 citation statements)

References 14 publications

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“…However, the particle size increased with increase in drug loading in agreement with earlier studies (Obitte et al, 2012;Umeyor et al, 2012;Brown et al, 2013;Chime et al, 2013a). Particle size of lipospheres determines the site of application of the formulation and also affects the bioavailability of the drug.…”

Section: Particle Size and Morphology Of Lipospheressupporting

confidence: 87%

“…Against these backdrops, there is an urgent need to develop highly efficacious formulations of artesunate to enhance its oral solubility and pharmacokinetic profiles. Liposphere drug delivery system is an emerging carrier for both hydrophilic and hydrophobic drugs (Brown et al, 2013). Lipospheres were first reported as a particulate dispersion of solid spherical particles between 0.2 and 100 mm in diameter consisting of solid hydrophobic fat core such as triglycerides or fatty acids derivatives, stabilised by monolayer of phospholipids (Domb and Manier, 1990;Chime et al, 2012a).…”

Section: Introductionmentioning

confidence: 99%

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Evaluation of dika wax-soybean oil-based artesunate-loaded lipospheres:in vitro–in vivocorrelation studies

Chinaeke

Chime

Ogbonna

et al. 2014

Journal of Microencapsulation

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Section: Particle Size and Morphology Of Lipospheressupporting

confidence: 87%

Section: Introductionmentioning

confidence: 99%

Evaluation of dika wax-soybean oil-based artesunate-loaded lipospheres:in vitro–in vivocorrelation studies

Chinaeke

Chime

Ogbonna

et al. 2014

Journal of Microencapsulation

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“…The encapsulation efficiency (EE%) of the drug in the microparticles was calculated from the equation: where TDC is the weight of drug added to the formulation, while ADC is the analyzed weight of the drug in the SLMs (Brown et al, 2013).…”

Section: Drug Content and Encapsulation Efficiency Analysismentioning

confidence: 99%

“…Plant and animal sources of lipids have been explored as potential excipients for lipid-based formulations Obitte et al, 2012;Brown et al, 2013). Although chemical specificity and purity may not be optimal, these lipids may be superior to synthetic forms as regards toxicity and biocompatibility (Obitte et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

“…Lipid-based formulations have been shown to enhance the bioavailability of drugs administered orally (Hou et al, 2003;You et al, 2005;Chime et al, 2012Chime et al, , 2013aBrown et al, 2013). Structured lipid matrices have been shown to have improved physical properties compared with the individual components and have the ability of combining the beneficial characteristics of component fatty acids.…”

Section: Introductionmentioning

confidence: 99%

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Formulation development and evaluation of the anti-malaria properties of sustained release artesunate-loaded solid lipid microparticles based on phytolipids

et al. 2014

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Contexts: Artemisinins and its derivatives are considered the basis in the treatment of Plasmodium falciparum malaria due to their high potency and rapid action. However, they have short half life, low solubility, and poor oral bioavailability, hence the need to formulate sustained release lipid particulate dosage form of these drugs. Objectives: To formulate and evaluate artesunate-loaded solid lipid microparticles (SLMs) based on structured lipid matrices consisting of soybean oil and dika wax. Materials and methods: The lipid matrices were characterized by differential scanning calorimetry (DSC), small-angle X-ray diffraction (SAXD), and wide-angle X-ray diffraction (WAXD). The SLMs were prepared by hot melt-homogenization. Time-dependent particle size analysis, time-dependent pH stability studies, encapsulation efficiency (EE%), and in vitro drug release were carried out on the SLMs. In vivo anti-malarial studies were performed using a modified Peter's 4-day suppressive protocol using Plasmodium berghei infected mice. Results and discussion: Thermograms of the lipid matrices showed modifications in the microstructure of dika wax as a result of inclusion of soybean oil. SAXD and WAXD diffractograms showed that the lipid matrices were found to be non-lamellar. Particle size of SLM increased with time, while the pH was almost constant. The SLMs had maximum EE% of 80.6% and sustained the release of artesunate more than the reference tablet. In vivo pharmacodynamic studies showed that the SLMs had significant (p50.05) reduction in parasitaemia compared with reference tablet. Conclusion: Artesunate-loaded SLMs could be used once daily in the treatment of malaria.

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Evaluation of the Properties of Encapsulated Stavudine Microparticulate Lipid-based Drug Delivery System in Immunocompromised Wistar Rats

Chime

Onunkwo

Attama

2020

CHR

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Background: Lipid based formulations have been confirmed to lower some side effects of drug and can be tailor made to offer sustained drug release of drugs with short half-life like stavudine. Aim: To evaluate the immunomodulatory properties of stavudine-loaded solid lipid microparticles (SLMs) using immunocompromised Wistar rats. Methods: The SLMs were formulated by homogenization method. The optimized batches were used for further in vivo studies. The effect of formulation on the CD4 count and the haematological properties of immunocompromised Wistar rats were studied. Results: The particle size range of 4 -8 µm, EE range of 85-93 % and maximum drug release at 10 h. The CD4 cells increased from 115 ± 3.17 cell/mm3 at day zero to 495 ± 5.64 cell/mm3 at day 14 of treatment and 538 ± 6.31 cell/mm3 at day 21. The red blood cells increased from 2.64 ± 1.58 (x 106 /mm3 ) at day zero to 6.96 ± 3.47 (x 106 /mm3 ) at day 14 and 7.85 ± 3.64 (x 106 /mm3 ) at day 21. PCV increased significantly (p < 0.05) to about 42 – 50 % at day 21 in the groups that received the SLMs formulations. The white blood cells (WBC) also were 12 x 103 /mm3 , for SLM formulations, while the rats that received plain stavudine exhibited WBC of 9.6 x 103 /mm3 at day 21. The histopathological studies revealed that oral stavudine-loaded SLMs had no significant damage to the kidney, liver, spleen and the brain of Wistar rats. Conclusion: Formulations exhibited significantly higher immunomodulatory properties than plain stavudine (p<0.05) and showed good properties for once daily oral administration and could be a better alternative to plain stavudine tablets for the management of patients living with HIV.

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<i>In vitro</i> and <i>In vivo</i> Characterisation of Piroxicam-Loaded Dika Wax Lipospheres

Cited by 7 publications

References 14 publications

Evaluation of dika wax-soybean oil-based artesunate-loaded lipospheres:in vitro–in vivocorrelation studies

Evaluation of dika wax-soybean oil-based artesunate-loaded lipospheres:in vitro–in vivocorrelation studies

Formulation development and evaluation of the anti-malaria properties of sustained release artesunate-loaded solid lipid microparticles based on phytolipids

Evaluation of the Properties of Encapsulated Stavudine Microparticulate Lipid-based Drug Delivery System in Immunocompromised Wistar Rats

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