Solid lipid microparticles produced by spray congealing: Influence of the atomizer on microparticle characteristics and mathematical modeling of the drug release

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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Formulation Design and Evaluation of Solid Lipid Micro-particles of Curcumin for the Treatment of Alzheimer’s disease

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i4.3610 ◽

2020 ◽

Vol 11 (4) ◽

pp. 6739-6747

Author(s):

Amin Mir M ◽

Muhammad Waqar Ashraf ◽

Maythem Mahmud

Keyword(s):

Drug Release ◽

Drug Loading ◽

Entrapment Efficiency ◽

Compatibility Study ◽

Cumulative Release ◽

Solid Lipid ◽

Micro Particles ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

Solid lipid microparticles reach the site of its action in a controlled rate and do show controlled release for a better therapeutic result. A good drug carrying and release system involve a controlled drug delivery that improves bioavailability, to enrich stability and to minimise the toxic effects followed with a targeted drug at the site of its action. The solid lipid microparticles of curcumin were prepared in a view to achieving high permeability of curcumin in the brain through blood-brain-barrier. The lipid microsphere solids were prepared by hot melts microencapsulation technique to formulate solid lipid microspheres. Twelve lipid formulations were prepared with varying concentration of surfactants (span 40, span 70, span 90 and Tween 100). The developed formulation was subjected to various parameters such as the particle size, % entrapment efficiencies, yield productions, % cumulative release, percentage yield and drug loading, based upon highest entrapment efficiency, drug release and % cumulative release, the F3 formulation was considered as the best formulation. The prepared microsphere was subjected to different evaluation parameters such as thin-layer chromatography, melting point, FTIR, solubility, compatibility study and In-vitro drug release. The developed formulation shows spherical and smooth surface. The percentage release of drug F3 formulation has been found highest of about 86.23% after 12 hr.

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Determination of Solid State Characteristics of Spray-Congealed Ibuprofen Solid Lipid Microparticles and Their Impact on Sustaining Drug Release

Molecular Pharmaceutics ◽

10.1021/acs.molpharmaceut.5b00015 ◽

2015 ◽

Vol 12 (5) ◽

pp. 1592-1604 ◽

Cited By ~ 14

Author(s):

Priscilla Chui Hong Wong ◽

Paul Wan Sia Heng ◽

Lai Wah Chan

Keyword(s):

Solid State ◽

Drug Release ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

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Solid lipid microparticles: formulation, preparation, characterisation, drug release and applications

Expert Opinion on Drug Delivery ◽

10.1517/17425247.2.1.75 ◽

2005 ◽

Vol 2 (1) ◽

pp. 75-87 ◽

Cited By ~ 101

Author(s):

Séverine Jaspart ◽

Géraldine Piel ◽

Luc Delattre ◽

Brigitte Evrard

Keyword(s):

Drug Release ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Lipid Microparticles

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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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