LIPID NANOPARTICLES FOR TRANSDERMAL DELIVERY OF CELECOXIB: AN IN VITRO AND IN VIVO INVESTIGATION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (08) ◽  
pp. 38-48
Author(s):  
S. V Shinde ◽  
S Nikam ◽  
P Raut ◽  
M. K. Ghag ◽  

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.

2020 ◽  
Vol 11 (1) ◽  
pp. 204-204
Author(s):  
Solmaz Ghaffari ◽  
Faezeh Alihosseini ◽  
Seyed Mahdi Rezayat Sorkhabadi ◽  
Sepideh Arbabi Bidgoli ◽  
Seyyedeh Elaheh Mousavi ◽  
...  

2018 ◽  
Vol 164 ◽  
pp. 332-339 ◽  
Author(s):  
Sara Daneshmand ◽  
Mahmoud Reza Jaafari ◽  
Jebrail Movaffagh ◽  
Bizhan Malaekeh-Nikouei ◽  
Mehrdad Iranshahi ◽  
...  

Author(s):  
PALLAVI M CHAUDHARI ◽  
VAISHNAVI M BIND

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.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Praveen Kumar Gaur ◽  
Shikha Mishra ◽  
Suresh Purohit

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.


2021 ◽  
Author(s):  
Mohhammad Ramzan ◽  
Samuel Gourion-Arsiquaud ◽  
Afzal Hussain ◽  
Jaspreet Singh Gulati ◽  
Qihong Zhang ◽  
...  

Abstract The study focused to optimize, evaluate and investigate mechanistic perspective of ketoconazole (KTZ) loaded solid lipid nanoparticles (KTZ-SLNs) for enhanced permeation across rat skin. KTZ-SLNs were evaluated for size, distribution, zeta potential (ZP), percent entrapment efficiency (%EE), drug release, morphology, thermal behavior (DSC), compatibility (FTIR) and solid state characterization (X-ray diffraction, XRD). Moreover, ex-vivo permeation and drug deposition into rat skin were conducted using Franz diffusion cell. Mechanistic evaluations were confirmed using confocal laser scanning microscopy and vibrational ATR methods using EpiDermTM model. An in vivo dermatokinetics study was performed to ensure KTZ access to the dermal region. Accelerated and photostability studies were conducted at different temperatures (0, 30, and 40 °C) for 12 months. The spherical optimized KOF1 showed optimal particle size (291 nm), and high negative ZP (-27.7 mV). Results of FTIR, DSC, and XRD confirmed compatibility of KTZ with excipients, purity of KTZ & dissolved KTZ in lipid matrix, and amorphous nature of KTZ-SLNs. In-vitro release was found to be slow and sustained whereas ex vivo permeation parameters were significantly high in KTZ-SLNs as compared to drug suspension and marketed product. Drug retention was 10- and -5 fold higher than KTZ-SUS and marketed product, respectively. Pharmacokinetic parameters were improved by SLNs formulation. Confocal raman spectroscopy experiment showed that KTZ-SLNs could penetrate beyond the human stratum corneum into viable epidermis. Fluorescent microscopy confirmed improved penetration of KTZ-SLNs was through human follicular pathway. KTZ-SLNs stable over 12 months under set conditions.


2018 ◽  
Vol 8 (3) ◽  
pp. 395-400 ◽  
Author(s):  
Solmaz Ghaffari ◽  
Faezeh Alihosseini ◽  
Seyed Mahdi Rezayat Sorkhabadi ◽  
Sepideh Arbabi Bidgoli ◽  
Seyyedeh Elaheh Mousavi ◽  
...  

2014 ◽  
Vol 21 (11) ◽  
pp. 1157-1162 ◽  
Author(s):  
Marina Gallarate ◽  
Loredana Serpe ◽  
Federica Foglietta ◽  
Gian Zara ◽  
Susanna Giordano ◽  
...  

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