Diazepam-Loaded Solid Lipid Nanoparticles: Design and Characterization

Abdelbary, Ghada A.; Fahmy, Rania Samir

doi:10.1208/s12249-009-9197-2

Cited by 196 publications

(94 citation statements)

References 30 publications

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“…This is in agreement with reports by Abdelbary et al and Kumar et al 42,43 The higher %EE and %DL found in formulations containing stearic acid either alone or in combination with other lipid material is obvious, and can be explained by the higher solubility of sulpiride in acids. 2,44 This was confirmed by the rapid dissolution of sulpiride in melted stearic acid during the preparation of SLN.…”

supporting

confidence: 93%

Novel sulpiride-loaded solid lipid nanoparticles with enhanced intestinal permeability

Ibrahim¹,

Alomrani²,

Yassin³

2013

IJN

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Background Solid lipid nanoparticles (SLN), novel drug delivery carriers, can be utilized in enhancing both intestinal permeability and dissolution of poorly absorbed drugs. The aim of this work was to enhance the intestinal permeability of sulpiride by loading into SLN. Methods A unique ultrasonic melt-emulsification method with minimum stress conditions was used for the preparation of SLN. The mixture of the drug and the melted lipids was simply dispersed in an aqueous solution of a surfactant at a temperature that was 10°C higher than the melting points of the lipids using probe sonication, and was then simultaneously dispersed in cold water. Several formulation parameters were optimized, including the drug-to-lipid ratio, and the types of lipids and surfactants used. The produced SLN were evaluated for their particle size and shape, surface charge, entrapment efficiency, crystallinity of the drug and lipids, and the drug release profile. The rat everted sac intestine model was utilized to evaluate the change in intestinal permeability of sulpiride by loading into SLN. Results The method adopted allowed successful preparation of SLN with a monodispersed particle size of 147.8–298.8 nm. Both scanning electron microscopic and atomic force microscopic images showed uniform spherical particles and confirmed the sizes determined by the light scattering technique. Combination of triglycerides with stearic acid resulted in a marked increase in zeta potential, entrapment efficiency, and drug loading; however, the particle size was increased. The type of surfactant used was critical for particle size, charge, drug loading, and entrapment efficiency. Generally, the in vitro release profile demonstrated by all formulations showed the common biphasic mode with a varying degree of burst release. The everted sac model showed markedly enhanced sulpiride permeability in the case of the SLN-loaded formulation. The in situ results showed a very good correlation with the in vitro release data. Conclusion Incorporation of sulpiride into SLN results in enhanced intestinal permeability of sulpiride, that may in turn increase overall oral absorption of the drug. The superior attributes of the prepared SLN, specifically the high particle size uniformity and drug loading capacity, is considered novel, especially given the simplicity and modest nature of the sonication method used.

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supporting

confidence: 93%

Novel sulpiride-loaded solid lipid nanoparticles with enhanced intestinal permeability

Ibrahim¹,

Alomrani²,

Yassin³

2013

IJN

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“…7 Furthermore, the ITZ-NLCs had a lessordered crystal structure, which would contribute to a higher drug-loading capacity. 39 A similar finding was reported by Chen et al for the XRD analysis of ITZ-loaded nanoparticles with human serum albumin. 7 The XRD of ITZ powder also showed sharp peaks, which demonstrated the existence of crystalline ITZ.…”

Section: Xrd Studysupporting

confidence: 82%

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

Lim¹,

Rajinikanth²,

Chitneni³

et al. 2014

IJN

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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.

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“…The data clearly showed that higher concentration of oil phase surfactant caused higher DL/EE and decreased the mean size of the SLNs. This notion previously has been shown (Abdelbary & Fahmy, 2009). This fact may attribute to the reduction of surface tension with higher lipophilic surfactant content that may lead to smaller particles (Hu et al, 2005).…”

Section: Discussionmentioning

confidence: 54%

Formulation, characterization, and geno/cytotoxicity studies of galbanic acid-loaded solid lipid nanoparticles

Eskandani

Barar

Dolatabadi

et al. 2015

Pharmaceutical Biology

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Context: Galbanic acid (GBA) is a sesquiterpene coumarin with different medicinal properties and anticancer effects. Objective: To improve the anticancer activities of GBA, in the current study, we aimed to fabricate GBA-loaded solid lipid nanoparticles (GBA-SLNs) and study their biological activities in vitro. Materials and methods: Hot homogenization was used for preparation of GBA-SLNs. The encapsulation efficiency (EE) and drug loading (DL) and in vitro release were determined. MTT, DAPI, DNA fragmentation, comet, and Anexin V apoptosis assays were used to compare the anti-cell proliferation and genotoxicity properties of GBA and GBA-SLNs against A549 cells and HUVEC to detect apoptosis and DNA damage in the final concentration of 100 mM after 48 h treatment. Results: Scanning electron microscopy (SEM) and particle size analysis showed spherical SLNs (92 nm), monodispersed distribution, and zeta potential of À23.39 mV. High EE (498%) and long-term in vitro release were achieved. The stability of GBA-SLNs in aqueous medium was approved after 3 months in terms of size and polydispersity index. GBA was able to inhibit A549 growth with an IC 50 value of 62 mM at 48 h. Although GBA-SLNs could also inhibit the growth rate of A549 cells, the effect is perceived after 48 h, as approved by the quantitative expression of Bcl-xL and Casp 9 genes, and also genotoxicity assays. Conclusion: Long-term apoptotic effect of GBA-SLNs compared with GBA may be due to the accumulation of GBA-SLNs in the tumor site because of deviant tumor pathology. Our data confirmed that SLNs could be exploited for sustained lipophilic GBA delivery.

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Diazepam-Loaded Solid Lipid Nanoparticles: Design and Characterization

Cited by 196 publications

References 30 publications

Novel sulpiride-loaded solid lipid nanoparticles with enhanced intestinal permeability

Novel sulpiride-loaded solid lipid nanoparticles with enhanced intestinal permeability

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

Formulation, characterization, and geno/cytotoxicity studies of galbanic acid-loaded solid lipid nanoparticles

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