Physicochemical Characterization of Artemether-Entrapped Solid Lipid Microparticles Prepared from Templated- Compritol and Capra hircus (Goat Fat) Homolipid

The purpose of this study was to formulate and evaluate the physicochemical properties of artemetherloaded solid lipid microparticles (SLM) prepared from templated-compritol 888®ATO and Capra hircus (goat fat) homolipid. Various ratios of compritol 888®ATO, goat fat and Phospholipon® 90G were used to prepare the templated lipid matrices and characterized by differential scanning calorimetry (DSC). Plain and artemether-loaded SLM (0, 1.0, 3.0 and 5.0% drug) were prepared by melt-homogenization. The SLM were characterized regarding the compatibility by DSC, morphology and particle size by polarized light microscopy (PLM), encapsulation efficiency (EE%), in vitro release in simulated gastric fluid (SGF, pH 1.2), simulated intestinal fluid (SIF, pH 7.2) and alcoholic buffer (pH 3.6), and time-resolved pH-dependent stability. Stable, smooth and mostly spherical SLM with particle sizes in the range 18.77-43.79 μm and EE% ranging from 62.22% to 99.05% were obtained. DSC results showed the compatibility of drug and the formulation excipients as well as the stability of artemether in the developed SLM. Results showed significantly (p<0.05) higher drug release (88.25%) in alcoholic buffer than in SIF and SGF. By implication, incorporation of alcohol in the formulation would be a practical approach to improve artemether bioavailability from the SLM. This study has shown that the physicochemical properties of artemether were improved by SLM based on templated-compritol 888®ATO and goat fat. Dhaka Univ. J. Pharm. Sci. 20(1): 67-80, 2021 (June)

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Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.1.3 ◽

2017 ◽

Vol 10 (1) ◽

pp. 3582-3593

Author(s):

Chukwuebuka Umeyor ◽

Uchechukwu Nnadozie ◽

Anthony Attama

Keyword(s):

Oral Delivery ◽

In Vitro Release ◽

Carrier System ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Release Study ◽

Lipid Microparticles ◽

Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

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Testosterone solid lipid microparticles for transdermal drug delivery. Formulation and physicochemical characterization

Journal of Microencapsulation ◽

10.1080/02652040701368865 ◽

2007 ◽

Vol 24 (5) ◽

pp. 457-475 ◽

Cited By ~ 21

Author(s):

Amal H. El-Kamel ◽

Iman M. Al-Fagih ◽

Ibrahim A. Alsarra

Keyword(s):

Drug Delivery ◽

Transdermal Drug Delivery ◽

Physicochemical Characterization ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

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Anti-Inflammatory and Gastroprotective Properties of Aspirin - Entrapped Solid Lipid Microparticles

Recent Patents on Inflammation & Allergy Drug Discovery ◽

10.2174/1872213x14666200108101548 ◽

2020 ◽

Vol 14 (1) ◽

pp. 78-88

Author(s):

Salome A. Chime ◽

Paul A. Akpa ◽

Cosmas C. Ugwuanyi ◽

Anthony A. Attama

Keyword(s):

Particle Size ◽

Drug Release ◽

Particle Size Range ◽

Simulated Intestinal Fluid ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles ◽

Anti Inflammatory ◽

Gastric Irritation

Background: Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529, 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation. Objective: The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance oral bioavailability and inhibit gastric irritation. Methods: This solid lipid microparticles loaded with aspirin (SLM) was formulated by a modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, Encapsulation Efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats. Results: The results showed that aspirin entrapped SLM exhibited the highest EE of 72% and particle size range of 7.60 + 0.141µm to 20.25 + 0.070µm. Formulations had about 55% drug release at 6h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100% gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage of anti-inflammatory activities also showed that aspirin-entrapped SLM had 78% oedema inhibition at 7h, while the reference had 68% inhibition at 7h. Conclusion: Aspirin-entrapped SLM showed good sustained-release properties, enhanced antiinflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.

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Evaluation of Gentamicin-Entrapped Solid Lipid Microparticles Formulated with a Biodegradable Homolipid from Capra hircus

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v13i8.2 ◽

2014 ◽

Vol 13 (8) ◽

pp. 1999 ◽

Cited By ~ 2

Author(s):

FC Kenechukwu ◽

CE Umeyor ◽

MA Momoh ◽

JDN Ogbonna ◽

SA Chime ◽

...

Keyword(s):

Capra Hircus ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

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Controlled release of indomethacin from crosslinked alginate beads

e-Polymers ◽

10.1515/epoly.2008.8.1.177 ◽

2008 ◽

Vol 8 (1) ◽

Cited By ~ 3

Author(s):

Murat Inal ◽

Mustafa Yiğitoğlu ◽

Nuran Işiklan

Keyword(s):

Sodium Alginate ◽

Exposure Time ◽

Alginate Bead ◽

In Vitro Release ◽

Alginate Beads ◽

Simulated Gastric Fluid ◽

Scanning Calorimetry ◽

Simulated Intestinal Fluid ◽

Release Data

AbstractBeads of the sodium alginate (NaAlg) were prepared by dropping aqueous sodium alginate (NaAlg) into glutaraldehyde (GA) as a crosslinker and HCl as a catalyst mixture solution. Beads prepared were used to deliver a model non-steroid, anti-inflammatory drug, indomethacin (IM). The beads were characterized with Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Chemical stability of the IM after encapsulation into beads was confirmed by FTIR. SEM photograph indicated that alginate bead has spherical shape and rough surface. Preparation conditions of the beads were optimized by considering the percentage of entrapment efficiency, swelling capacity of the beads, particle size and their release data. In vitro release studies were performed in simulated gastric fluid (pH 1.2) for the initial 2 h, followed by simulated intestinal fluid (pH 7.4) for 4 h. Effects of variables such as, GA concentration, exposure time to GA, drug/polymer (d/p) ratio and percentage of HCl on the release of the IM were investigated. It was observed that, IM release from the beads decreased with increasing GA concentration, exposure time to GA, d/p ratio and percentage of HCl. The highest cumulative IM release obtained at the end of 6 h was 68% for alginate beads which were prepared with 0.5% HCl. On the other hand the least cumulative IM release obtained was to be 20 % for alginate beads which were prepared with 30 min exposure time to GA. In order to understand the crosslinking of the polymeric matrix, the molar mass between crosslinks were calculated using the swelling parameters. It was also found from the swelling experiments that swelling degree of the beads increases with increase in the temperature. The release data have been fitted to an empirical equation to estimate the kinetic parameters. The diffusion coefficient was also calculated for the transport of the drug through the polymeric beads. Values of these parameters were found to be consistent with the release data.

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Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy

Pharmaceutics ◽

10.3390/pharmaceutics11080364 ◽

2019 ◽

Vol 11 (8) ◽

pp. 364 ◽

Cited By ~ 3

Author(s):

Bertoni ◽

Albertini ◽

Facchini ◽

Prata ◽

Passerini

Keyword(s):

Delivery System ◽

Oral Drug Delivery ◽

In Vitro Release ◽

Radical Scavenging ◽

Antioxidant Therapy ◽

Oral Drug ◽

Solid Lipid ◽

Antioxidant Agents ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were produced by spray congealing technology. The obtained SLMs had main particle sizes ranging from 250 to 355 µm, suitable for oral administration. GSH was efficiently loaded into the SLMs at 5% or 20% w/w and the encapsulation process did not modify its chemico-physical properties, as demonstrated by FT-IR, DSC and HSM analysis. Moreover, in vitro release studies using biorelevant media showed that Dynasan 114-based SLMs could efficiently release GSH in various intestinal fluids, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay demonstrated the good radical scavenging activity of this formulation. Dynasan 114-based SLMs exhibited an excellent biocompatibility on intestinal HT-29 cells at concentrations up to 2000 μg/mL. SLMs containing GSH alone or together with another antioxidant agent (catalase) were effective in reducing intracellular reactive oxygen species (ROS) levels. Overall, this study indicated that spray congealed SLMs are a promising oral drug delivery system for the encapsulation of one or more biological antioxidant agents for local intestinal treatment.

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Sustained release biodegradable solid lipid microparticles: Formulation, evaluation and statistical optimization by response surface methodology

Acta Pharmaceutica ◽

10.1515/acph-2017-0034 ◽

2017 ◽

Vol 67 (4) ◽

pp. 441-461

Author(s):

Muhammad Hanif ◽

Hafeez Ullah Khan ◽

Samina Afzal ◽

Asif Mahmood ◽

Safirah Maheen ◽

...

Keyword(s):

Entrapment Efficiency ◽

Quadratic Model ◽

Release Mechanism ◽

Scanning Calorimetry ◽

Glyceryl Monostearate ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles ◽

The Impact ◽

Central Composite

Abstract For preparing nebivolol loaded solid lipid microparticles (SLMs) by the solvent evaporation microencapsulation process from carnauba wax and glyceryl monostearate, central composite design was used to study the impact of independent variables on yield (Y1), entrapment efficiency (Y2) and drug release (Y3). SLMs having a 10-40 μm size range, with good rheological behavior and spherical smooth surfaces, were produced. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry pointed to compatibility between formulation components and the zeta-potential study confirmed better stability due to the presence of negative charge (-20 to -40 mV). The obtained outcomes for Y1 (29-86 %), Y2 (45-83 %) and Y3 (49-86 %) were analyzed by polynomial equations and the suggested quadratic model were validated. Nebivolol release from SLMs at pH 1.2 and 6.8 was significantly (p < 0.05) affected by lipid concentration. The release mechanism followed Higuchi and zero order models, while n > 0.85 value (Korsmeyer- Peppas) suggested slow erosion along with diffusion. The optimized SLMs have the potential to improve nebivolol oral bioavailability.

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