Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium

Attama, Anthony A.; Okafor, C. E.; Builders, Philip F.; Okorie, O

doi:10.3109/10717540903334959

Cited by 65 publications

(81 citation statements)

References 21 publications

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“…While the latter component, being a hydrophilic surfactant promoted the solubilization of gentamicin within the core lipid matrix, the former gave rise to the formation of structured lipid matrices, which improved the entrapment of the drug in the core of the preparations. [24,32]. The increase observed in the formulations is suggestive of their possible employment as sustained release delivery system.…”

Section: Resultsmentioning

confidence: 83%

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

Adedokun

Jackson

Uchegbu

et al. 2017

Int J Pharm Pharm Sci

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Objective: Despite the broad pharmacological activity of gentamicin against a number of bacteria, it's very inadequate oral bioavailability due to poor intestinal membrane permeability has limited its formulation into oral dosage delivery system. This work was thus aimed at formulation and evaluation of gentamicin-loaded microemulsions based on preparation of lipid matrix for sustained release delivery. Methods:Oral gentamicin suspensions were prepared by emulsification method using Tween 80 as a mobile surfactant in the lipid matrix dispersion. The resultant oral suspensions were evaluated for mean particle size and morphology using a photomicrograph, encapsulation efficiency/entrapment, EE (%), dispersibility, pH and absolute drug content. Release study as a function of inhibition zone diameter (IZD) and in vitro release study was also carried out. The in vitro release study was performed in both simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.2) respectively. The release data were analyzed mathematically according to zero order, first order and Higuchi equations. Results:The prepared suspensions were cream-white in colour, easily dispersed and well homogenized. Batch D, which had least amount of excipients incorporated into the lipid matrix showed clumped irregular-shaped and less free-flowing particles. The particle size was significantly influenced by lipid matrix combination ratio in the presence of a surfactant (p<0.05). The mean particle size diameters of the samples were 15.44 mm, 10.64 mm, 4.12 mm, and 2.70 mm for batches A, B, C and D respectively. The values of EE obtained varied between 47% and 59% with Batch B exhibiting the highest value. The Higuchi model gave the best release kinetics result followed by zero order kinetics. Conclusion:Oral gentamicin prepared exhibited antibacterial properties against Klebsiella spp., Escherchia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. The results suggest that a lipid matrix system could be useful as a sustained release oral delivery system of a poorly absorbable drug such as gentamicin.

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Section: Resultsmentioning

confidence: 83%

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

Adedokun

Jackson

Uchegbu

et al. 2017

Int J Pharm Pharm Sci

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“…Change in pH could be a function of degradation of the active pharmaceutical ingredient (API) or excipients. A prior stable API may be affected by degradation of excipients with storage through generation of unfavorable pH (increase or decrease) or reactive species for the API (Chime et al, 2012;Attama et al, 2009).…”

Section: Time Dependent Ph Stabilitymentioning

confidence: 99%

Application of Ipomoea batatas starch as suspending agent in acetaminophen suspension

Ikechukwu¹,

A²,

Ifeoma³

2014

Afr. J. Pharm. Pharmacol.

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“…Loading capacity (LC) expresses the ratio between the entrapped active pharmaceutical ingredient (API) and the total weight of the lipids (Attama et al, 2009;Umeyor et al, 2012;Chime et al, 2013aChime et al, , 2013b. LC was determined using the relationship:…”

Section: Drug Loading Capacitymentioning

confidence: 99%

“…The artesunate-loaded SLMs were prepared using the hot melt homogenization technique (Attama et al, 2009) according to the formula presented in Table 1. In each case, 10 g of the lipid matrix was melted at 70 C on a water bath and an appropriate amount of artesunate was incorporated into the lipidic melt.…”

Section: Formulation Of the Microparticlesmentioning

confidence: 99%

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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Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium

Cited by 65 publications

References 21 publications

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

Application of Ipomoea batatas starch as suspending agent in acetaminophen suspension

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

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