Application of quality by design approach for intranasal delivery of rivastigmine loaded solid lipid nanoparticles: Effect on formulation and characterization parameters

Shah, Brijesh; Khunt, Dignesh; Bhatt, Himanshu; Misra, Manju; Padh, Harish

doi:10.1016/j.ejps.2015.07.002

Cited by 183 publications

(83 citation statements)

References 44 publications

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“…37,38 On the other hand, X 1 had a negative effect on Y 5 which could be explained by increasing the particle size and subsequently decreasing the specific surface area and, …”

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confidence: 99%

Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study

Badawi¹,

Teaima²,

El-Say³

et al. 2018

IJN

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Background Pomegranate extract (PE) is a natural product with potent antioxidant and anticancer activity because of its polyphenols content. The main purpose of this study was to maximize the PE chemotherapeutic efficacy by loading it in an optimized solid lipid nanoparticles (SLNs) formula. Materials and methods The influence of independent variables, which were lipid concentration (X 1 ), surfactant concentration (X 2 ) and cosurfactant concentration (X 3 ), on dependent ones, which were particle size (Y 1 ), polydispersity index (Y 2 ), zeta potential (Y 3 ), entrapment efficiency (Y 4 ) and cumulative % drug release (Y 5 ), were studied and optimized using the Box–Behnken design. Fifteen formulations of PE-SLNs were prepared using hot homogenization followed by ultra-sonication technique. Response surface plots, Pareto charts and mathematical equations were produced to study the impact of independent variables on the dependent quality parameters. The anti-proliferative activity of the optimized formula was then evaluated in three different cancer cell lines, namely, MCF-7, PC-3 and HepG-2, in addition to one normal cell line, HFB-4. Results The results demonstrated that the particle sizes ranged from 407.5 to 651.9 nm and the entrapment efficiencies ranged from 56.02 to 65.23%. Interestingly, the 50% inhibitory concentration of the optimized formula had more than a 40-fold improved effect on the cell growth inhibition in comparison with its free counterpart. Furthermore, it was more selective against cancer cells than normal cells particularly in MCF-7 breast cancer cells. Conclusion These data proved that nanoencapsulation of PE enhanced its anticancer efficacy. Therefore, our results suggested that a PE-loaded SLNs optimized-formula could be a promising chemo therapeutic agent.

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“…37,38 On the other hand, X 1 had a negative effect on Y 5 which could be explained by increasing the particle size and subsequently decreasing the specific surface area and, …”

mentioning

confidence: 99%

Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study

Badawi¹,

Teaima²,

El-Say³

et al. 2018

IJN

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“…The particle size of the prepared SLN was in the range of 69-223 nm, where the smallest particles were obtained after sonication treatment. Moreover, the examined SLN were characterized by PI values around 0.4 suggesting a broad distribution of the same particles [25]. All zeta potential values were found negative, but in the case of SLN formulated starting from acetic phase the external charge of the SLN was slightly negative for both GSH-SLN (HAc), and sonicated GSH-SLN (HAc), (-4.0 mV and -2.5 mV, respectively).…”

Section: Discussionmentioning

confidence: 95%

“…the exclusion of any chemical modification of GSH, by monitoring its HPLC peak before and after each sonication treatment. In the literature, several examples of sonication applied to solid lipid nanoparticles are reported, either for loading of hydrophilic drug substances [25,29] or hydrophobic ones [30][31][32]. Herein, we have tried to pre-form SLN according to the melt-emulsification technique and as a following step to apply probe-sonication, in an attempt to protect the sensitive molecule of GSH inside a preformed SLN carrier.…”

Section: Discussionmentioning

confidence: 99%

Glutathione loaded solid lipid nanoparticles: Preparation and in vitro evaluation as delivery systems of the antioxidant peptide to immunocompetent fish cells

Trapani

Tripodo

Mandracchia

et al. 2016

JCB

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“…[92][93][94][95][96] Initially, SLN-or MSLN-loaded bioactive compounds were given intranasally or intravenously, and these showed extensive bioavailability in the brain, thereby preventing inflammation and further progression of AD. [97][98][99][100][101] Quercetin-loaded SLN with a particle size of about 200 nm was studied for its efficacy in the AD model, and it showed excellent delivery of quercetin to the brain with a higher antioxidative effect in brain cells. 102 The transport of bioactive compounds to the brain occurs through the endocytosis of the brain capillaries, and these compounds can thereby cross the blood-brain barrier.…”

Section: Anti-alzheimer's Effectmentioning

confidence: 99%

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

Ganesan

Ramalingam

Karthivashan

et al. 2018

IJN

127

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Solid lipid nanoparticle (SLN) delivery systems have a wide applicability in the delivery of phyto-bioactive compounds to treat various chronic diseases, including diabetes, cancer, obesity and neurodegenerative diseases. The multiple benefits of SLN delivery include improved stability, smaller particle size, leaching prevention and enhanced lymphatic uptake of the bioactive compounds through oral delivery. However, the burst release makes the SLN delivery systems inadequate for the oral delivery of various phyto-bioactive compounds that can treat such chronic diseases. Recently, the surface-modified SLN (SMSLN) was observed to overcome this limitation for oral delivery of phyto-bioactive compounds, and there is growing evidence of an enhanced uptake of curcumin delivered orally via SMSLNs in the brain. This review focuses on different SLN and SMSLN systems that are useful for oral delivery of phyto-bioactive compounds to treat various chronic diseases.

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Application of quality by design approach for intranasal delivery of rivastigmine loaded solid lipid nanoparticles: Effect on formulation and characterization parameters

Cited by 183 publications

References 44 publications

Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study

Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study

Glutathione loaded solid lipid nanoparticles: Preparation and in vitro evaluation as delivery systems of the antioxidant peptide to immunocompetent fish cells

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

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