Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles

Kumari, Priyanka; Sathali, A. Abdul Hasan

doi:10.4103/0975-1483.100016

Cited by 65 publications

(35 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The burst release rate was affected by the change of concentration of lipid and surfactant in external phase. When the lipid concentration increased, the initial burst release rate decreased this may be due to the higher concentration of drug presence in the inner core (Priyanka & Sathali, 2012;Tsukamoto et al, 2013). The lipophilic nature of the CAR could be the reason for sustained release of the drug from internal lipid phase after initial burst release.…”

Section: In Vitro Release Kineticsmentioning

confidence: 99%

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

et al. 2016

View full text Add to dashboard Cite

The purpose of this study was to develop Carvedilol nanostructured lipid carriers (CAR-NLCs) using stearic acid and oleic acid as lipid, and to estimate the potential as oral delivery system for poorly water soluble drug. The particle-size analysis revealed that all the developed formulations were within the nanometer range. The EE and loading were found to be between 69.45-88.56% and 9.58-12.56%, respectively. The CAR-NLCopt showed spherical morphology with smooth surface under transmission electron microscope (TEM). The crystallization of the drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC) and revealed that the drug was in an amorphous state in the NLC matrix. The ex vivo gut permeation study showed many folds increment in the permeation of CAR-NLCs compared to Carvedilol suspension (CAR-S). The oral bioavailability study of CAR was carried out using Wistar rats and relative bioavailability of CAR-NLCopt was found to be 3.95 fold increased in comparison with CAR-S. In vivo antihypertensive study in Wistar rats showed significant reduction in mean systolic BP by CAR-NLCopt vis-à-vis CAR-S (p50.05) owing to the drug absorption through lymphatic pathways. In conclusion, the NLC formulation remarkably improved the oral bioavailability of CAR and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs. The promising findings in this investigation suggest the practicability of these systems for the enhancement of bioavailability of CAR.

show abstract

Section: In Vitro Release Kineticsmentioning

confidence: 99%

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

et al. 2016

View full text Add to dashboard Cite

show abstract

“…During the cooling phase, the drug is repartitioned into the lipid phase, and the solid lipid recrystallizes and forms a solid lipid core. 41 Greater amounts of the drug are entrapped in the core lipid matrix and lower amounts of the drug are deposited at the shell and/or the surface of the lipid nanoparticles. 42 Therefore, the formulation contains less amount of drug on the surface and the outer shell of the NLC contributes to the initial slow release; moreover, the drug present in the core of the lipid matrix contributes to the second fast release phase.…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Rajinikanth¹,

Chellian²

2016

IJN

View full text Add to dashboard Cite

The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol ® ATO 5 (glyceryl palmitostearate) and Labrasol ® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol ® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol ® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, −21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 μg/cm 2 /h) as compared with plain 5-FU gel (2.85±1.12 μg/cm 2 /h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 μg/cm 2 ) as compared with that from the 5-FU plain gel (12.23±3.86 μg/cm 2 ) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations.

show abstract

“…All three lipids exhibited a burst release within 30 minutes, followed by sustained release. 42 Based on the in vitro release results, we hypothesized that ITZ-NLCs were more likely to be the shell-enriched model, because most of the drug molecules were encapsulated at the lipid outer layer, which resulted in the immediate release followed by a slower release from the drug molecules in the lipid core.…”

mentioning

confidence: 99%

Formulation and delivery of itraconazole to the brain using a nanolipid carrier system

Lim¹,

Rajinikanth²,

Chitneni³

et al. 2014

IJN

View full text Add to dashboard Cite

The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol ® ATO 5 and Transcutol ® HP were selected as the lipid phase, and Tween ® 80 and Solutol ® HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, −18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.

show abstract

Preparation and Evaluation of Montelukast Sodium Loaded Solid Lipid Nanoparticles

Cited by 65 publications

References 10 publications

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Formulation and delivery of itraconazole to the brain using a nanolipid carrier system

Contact Info

Product

Resources

About