Fluticasone propionate–loaded solid lipid nanoparticles with augmented anti-inflammatory activity: optimisation, characterisation and pharmacodynamic evaluation on rats

In the present research work, celecoxib (CXB) loaded solid lipid nanoparticles (SLNs) were prepared using the probe sonication method, wherein Glyceryl monostearate and Tween 80 were used as solid lipid and surfactant, respectively. To obtain the statistically optimized batch, 32 factorial design was applied. The optimized batch was characterized physicochemically and evaluated through DSC, SEM and XRD studies. The mean particle size of the optimized batch was found to be 135.41± 0.24 nm with a mean % entrapment efficiency of 80 ± 1.69%. The optimized batch was further lyophilized and dispersed into 1% w/v Carbopol 934P to form a gel. Prepared gel was further evaluated for in vitro drug release, occlusivity, ex vivo permeability, local toxicity, in vivo anti-inflammatory activity and accelerated stability study. The study resulted in stable, safe and prolonged anti-inflammatory activity with quick onset of action. Hence, celecoxib loaded solid lipid nanoparticles can be considered as promising alternative to conventional topical systems.

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TOPICAL SOLID LIPID NANOPARTICLES BASED GEL OF LAVENDER ESSENTIAL OIL FOR ANTI‑INFLAMMATORY ACTIVITY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i11.35459 ◽

2019 ◽

pp. 175-182

Author(s):

PALLAVI M CHAUDHARI ◽

VAISHNAVI M BIND

Keyword(s):

Particle Size ◽

Drug Release ◽

Essential Oil ◽

Solid Lipid Nanoparticles ◽

Ex Vivo ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Inflammatory Activity ◽

Solid Lipid ◽

Anti Inflammatory

Objective: The main objective of the study was to formulate and evaluate and perform an optimization study of lavender essential oil loaded solid lipid nanoparticles (SLNs) based gel. Materials and Methods: SLNs were prepared by the hot homogenization technique. A total of eight formulations were formulated as per 23 factorial design by design expert 11 software. The formulated SLNs were further evaluated for particle size, entrapment efficiency, drug release profile. After evaluation, the optimized batch was further used for formulating gel. The formulated gel was further subjected to ex vivo studies. Results: After the evaluation of all the parameters, batch 7 was found to be optimized. Batch 7 was found to have the lowest particle size of 30.91±0.30, higher entrapment efficiency of 89.99±0.87, and higher drug release of 90.41±0.55. It was further used for formulating gel which was found to be consistent, homogenous, smooth, and spreadable. The % inhibition of the formulated SLN based gel was found to be 28±0.1%. Conclusion: The SLNs were prepared and were formulated into the gel. The gel showed anti-inflammatory activity.

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Solid Lipid Nanoparticles of Guggul Lipid as Drug Carrier for Transdermal Drug Delivery

BioMed Research International ◽

10.1155/2013/750690 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 18

Author(s):

Praveen Kumar Gaur ◽

Shikha Mishra ◽

Suresh Purohit

Keyword(s):

Drug Release ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Inflammatory Activity ◽

Physical Parameters ◽

In Vitro Drug Release ◽

Solid Lipid ◽

Lipid Component ◽

Anti Inflammatory

Diclofenac sodium loaded solid lipid nanoparticles (SLNs) were formulated using guggul lipid as major lipid component and analyzed for physical parameters, permeation profile, and anti-inflammatory activity. The SLNs were prepared using melt-emulsion sonication/low temperature-solidification method and characterized for physical parameters, in vitro drug release, and accelerated stability studies, and formulated into gel. Respective gels were compared with a commercial emulgel (CEG) and plain carbopol gel containing drug (CG) for ex vivo and in vivo drug permeation and anti-inflammatory activity. The SLNs were stable with optimum physical parameters. GMS nanoparticle 1 (GMN-1) and stearic acid nanoparticle 1 (SAN-1) gave the highest in vitro drug release. Guggul lipid nanoparticle gel 3 (GLNG-3) showed 104.68 times higher drug content than CEG in receptor fluid. The enhancement ratio of GLNG-3 was 39.43 with respect to CG. GLNG-3 showed almost 8.12 times higherCmaxthan CEG at 4 hours. The AUC value of GLNG-3 was 15.28 times higher than the AUC of CEG. GLNG-3 showed edema inhibition up to 69.47% in the first hour. Physicochemical properties of major lipid component govern the properties of SLN. SLN made up of guggul lipid showed good physical properties with acceptable stability. Furthermore, it showed a controlled drug release profile along with a promising permeation profile.

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Solid Lipid Nanoparticles Loaded with Fluorescent-labelled Cyclosporine A: Anti-Inflammatory Activity In Vitro

Protein and Peptide Letters ◽

10.2174/0929866521666140806164410 ◽

2014 ◽

Vol 21 (11) ◽

pp. 1157-1162 ◽

Cited By ~ 5

Author(s):

Marina Gallarate ◽

Loredana Serpe ◽

Federica Foglietta ◽

Gian Zara ◽

Susanna Giordano ◽

...

Keyword(s):

Cyclosporine A ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Inflammatory Activity ◽

Solid Lipid ◽

Anti Inflammatory

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Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

AAPS PharmSciTech ◽

10.1208/s12249-020-01807-9 ◽

2020 ◽

Vol 21 (7) ◽

Author(s):

Seyed Sadegh Shahraeini ◽

Jafar Akbari ◽

Majid Saeedi ◽

Katayoun Morteza-Semnani ◽

Shidrokh Abootorabi ◽

...

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Solid Lipid Nanoparticles ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Solid Lipid ◽

Inflammatory Agent ◽

Drug Entrapment Efficiency ◽

Anti Inflammatory ◽

Dermal Delivery

Abstract In the current research, the main focus was to overcome dermal delivery problems of atorvastatin. To this end, atorvastatin solid lipid nanoparticles (ATR-SLNs) were prepared by ultra-sonication technique. The prepared SLNs had a PDI value of ≤ 0.5, and the particle size of nanoparticles was in the range 71.07 ± 1.72 to 202.07 ± 8.40 nm. It was noticed that, when the concentration of lipid in ATR-SLNs increased, the size of nanoparticles and drug entrapment efficiency were also increased. Results showed that a reduction in the HLB of surfactants used in the preparation of SLN caused an increase in the particle size, zeta potential (better stability), and drug entrapment efficiency. Despite Tween and Span are non-ionic surfactants, SLNs containing these surfactants showed a negative zeta potential, and the absolute zeta potential increased when the concentration of Span 80 was at maximum. DSC thermograms, FTIR spectra, and x-ray diffraction (PXRD) pattern showed good incorporation of ATR in the nanoparticles without any chemical interaction. In vitro skin permeation results showed that SLN containing atorvastatin was capable of enhancing the dermal delivery of atorvastatin where a higher concentration of atorvastatin can be detected in skin layers. This is a hopeful promise which could be developed for clinical studies of the dermal delivery of atorvastatin nanoparticles as an anti-inflammatory agent.

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Solid lipid nanoparticles delivering anti-inflammatory drugs to treat inflammatory bowel disease: Effects in anin vivomodel

World Journal of Gastroenterology ◽

10.3748/wjg.v23.i23.4200 ◽

2017 ◽

Vol 23 (23) ◽

pp. 4200 ◽

Cited By ~ 18

Author(s):

Chiara Dianzani ◽

Federica Foglietta ◽

Benedetta Ferrara ◽

Arianna Carolina Rosa ◽

Elisabetta Muntoni ◽

...

Keyword(s):

Inflammatory Bowel Disease ◽

Bowel Disease ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Solid Lipid ◽

Inflammatory Bowel ◽

Inflammatory Drugs ◽

Anti Inflammatory

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Long-term Stable Cationic Solid Lipid Nanoparticles for the Enhanced Intracellular Delivery of SMAD3 Antisense Oligonucleotides in Activated Murine Macrophages

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/j3z312 ◽

2012 ◽

Vol 15 (3) ◽

pp. 467 ◽

Cited By ~ 5

Author(s):

Su-Eon Jin ◽

Chong-Kook Kim

Keyword(s):

Solid Lipid Nanoparticles ◽

Antisense Oligonucleotides ◽

Lipid Nanoparticles ◽

Homogenization Method ◽

Tween 20 ◽

Solid Lipid ◽

Intracellular Activity ◽

Macrophage Cells ◽

Anti Inflammatory

Purpose: Long-term stable cationic solid lipid nanoparticles (cSLNs) were formulated to transfer SMAD3 antisense oligonucleotides (ASOs) into the cells to enhance the intracellular activity of the ASOs. The SMAD3 ASOs were designed to block the inflammatory processes linked to TGFβ/SMAD3 pathway. Methods: The cSLN formulation was prepared by high-pressure homogenization method composed of 1,2-dioleoyl-3-trimethylammonium propane (DOTAP), dioleoylphosphoethanolamine (DOPE), Tween 20, and tricaprin as a solid lipid core (1:1:1:1.67, w/w). The size and the zeta potential of the prepared cSLNs were measured by light scattering. The cSLN/ASO complexes were generated and introduced into the murine macrophage cells. After the treatment of the complexes, the cellular uptake of the complexes was determined by flow cytometry and the intracellular activity of SMAD3 ASOs from the complexes was evaluated by western blotting of SMAD3. In addition, TGFβ1, an upstream molecule of TGFβ/SMAD3 pathway, was monitored by ELISA. Results: The nano-scale sized cSLNs were positively charged and physically stable at 4oC during the storage up to 24 months. The uptake efficiency of the cSLN/ASO complexes into macrophage cells was enhanced up to 80% without cytotoxicity. After the treatment of the cSLN/ASO complexes, SMAD3 as well as TGFβ1 was significantly suppressed based on the SMAD3 ASO activity in the macrophage cells. In addition, the cSLN/ASO complexes prevented the morphological change to dendritic shape in the activated macrophage cells. Conclusion: These results suggest that the cSLNs have a potential to deliver the SMAD3 ASOs to intracellular compartments for the anti-inflammatory effect. The development of this strategy might lead to anti-inflammatory and anti-fibrotic therapies in immunological disorders. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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