Surface modification of solid lipid nanoparticles for oral delivery of curcumin: Improvement of bioavailability through enhanced cellular uptake, and lymphatic uptake

Baek, Jong-Suep; Cho, Cheong-Weon

doi:10.1016/j.ejpb.2017.04.013

Cited by 170 publications

(95 citation statements)

References 30 publications

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“…For example, methoxy poly (ethylene glycol) poly (ε-caprolactane) nanoparticles have been shown to effectively deliver the curcumin with heightened oral bioavailability [25]. The PLGA and PEG coated curcumin was found to show higher efficiency and faster cellular uptake than the NC [26]. Likewise, encapsulation of curcumin with solid lipid nanoparticles resulted in an enhanced stability and biocompatibility [27].…”

Section: Discussionmentioning

confidence: 99%

Hepato therapeutic Efficacy of Native Curcumim and Nano –curcumin : A Novel Therapy Against Hyperthyroidism Induced Liver Oxidative and Inflammatory Damage in Rats

Al-Bishri¹

2017

Int. J. Adv. Res. Biol. Sci.

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Recent works have indicated the beneficial efficacy of using nanocurcumin in addressing poor bioavailability commonly associated with native curcumin. Curcumin has been shown to alleviate hyperthyroidism induced liver dysfunction. Here we carried out a comparative study using both native curcumin and nanocurcumin to verify the superior effects of encapsulation of curcumin in nanomaterials in blunting liver dysfunction in L-thyroxine induced hyperthyroid rats. Native curcumin (NC) and poly (lactide-co-glycolic acid (PLGA) encapsulated curcumin (PNC) significantly increased liver catalase activity and reduced glutathione (GSH) levels and significantly declined malondialdehyde (MDA) levels in hyperthyroid rats. However, rats treated with PNC had significantly better ameliorative effects on these parameters than rats treated with NC. Similarly, PNC showed significantly improved effects in lowering inflammatory mediators including TNF-a, IL-6, VEGF, CRP and caspase protein levels compared to NC in hyperthyroid rats. Serum T3, T4, and TSH levels and liver functional markers including albumin, ALT, ASP and AST were better controlled in PNC treated rats than in NC treated hyperthyroid rats. DNA fragmentation as estimated by comet assay was significantly lower in PNC treated rats than in NC treated rats. Likewise, significantly fewer histopathological and ultrastructural changes were observed in liver tissue in PNC treated hyperthyroid rats. Conclusion: Our work illustrates the capability of PNC to resolve hyperthyroidism induced liver dysfunction and substantiate the findings that beneficial effects of curcumin may be maximized by improving its stability and bioavailability by its encapsulation in nanoparticles.

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Section: Discussionmentioning

confidence: 99%

Hepato therapeutic Efficacy of Native Curcumim and Nano –curcumin : A Novel Therapy Against Hyperthyroidism Induced Liver Oxidative and Inflammatory Damage in Rats

Al-Bishri¹

2017

Int. J. Adv. Res. Biol. Sci.

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“…The uptake by the lymphatic cells and the oral bioavailability of the curcumin were found to be 6.3 and 9.5 times higher than that of curcumin suspension. 176 Based on the above studies, we can confirm that chitosan derivatives can be extensively used to improve the delivery of the phyto-bioactive compounds against various chronic diseases (Table 1).…”

Section: Chitosan-based Surface Modification Of Sln Delivery Systemsmentioning

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

133

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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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“…The list of some counter-ions and surface modifiers are shown in Table 2 11 . Surface modification using counter-ions and surface modifiers elaborates the new physicochemical properties of SLN 11 .The coating of a polymer on the SLN surface improves the stability of SLN in acidic medium and prevents the burst release of drug 24 . The quarternized chitosan derivative can be used for the protection of drug from acidic medium and further to stabilize the SLN.…”

Section: Other Agentsmentioning

confidence: 99%

“…The quarternized chitosan derivative can be used for the protection of drug from acidic medium and further to stabilize the SLN. The curcumin-loaded SLN coated with N-carboxymethyl chitosan (NCC) by surface charge interaction prevented the immediate release of curcumin in acidic medium and improved its bioavailability 24…”

Section: Other Agentsmentioning

confidence: 99%

“…In this method, SLN are prepared by using sonicator or high speed homogenizer. The combination of both techniques can also be used to get smaller particle size 24 . In a study, SLN of non-steroidal anti-inflammatory drugs were prepared using ultra-sonication assisted nano-emulsion method to get the nano-sized emulsion.…”

Section: Ultra-sonication/high Speed Homogenizationmentioning

confidence: 99%

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Solid lipid nanoparticles: a promising technology for delivery of poorly water-soluble drugs

Bhatt¹,

Sharma²,

Singh³

et al. 2018

actapharm

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Oral administration of drugs having low water solubility is hampered by various enzymatic barriers present in gastrointestinal (GI) tract. Lipid nanoparticles based on solid matrix have emerged as a potential drug delivery system to improve the absorption and bioavailability of several drugs, especially lipophilic compounds. Solid lipid nanoparticles (SLN) are reported as the most promising technology for oral administration and offered several advantages over conventional dosages formulations including, enhancement in solubility, stability, permeability, and bioavailability with minimal side effects. In this review, we have highlighted recent advances in the development of SLN for the oral, parenteral, rectal, and topical administration of various drugs. We have also summarized the applications of SLN in the treatment of various diseases like tuberculosis, cancer, diabetes, and several nervous system related disorders. sustained release, timed release, extended release, and targeted release of a drug. The predominance of nanoparticles over the other drug delivery systems enables them to use for drug targeting. Nanoparticles are 10-100nm in size in which drug is either dispersed or entrapped in a matrix, encapsulated as the solid solution or may be adsorbed on the surface 2 .The nanoparticles are designed to provide intimate contact with GI epithelium, prolong residence time and allow permeation across the cell membrane. A pre-systemic metabolism of a drug can be avoided by using nanoparticles 3 . Lipid nanoparticles are safe to use as they contain lipids, which are included in the category of generally recognized as safe (GRAS). Solid Lipid NanoparticlesSolid lipid nanoparticles are an advanced and rapidly budding field of nanotechnology with several applications in pharmaceutical science. SLN were developed first in 1991. These are the colloidal carriers possesses an average diameter of 10 to 1000nm. They composed of single lipid core matrix dispersed in an aqueous surfactant solution. The carriers like liposomes, polymeric micelles, and porous solids can also be used to enhance the aqueous solubility of a drug. But SLN not only helps to increase the solubility of a drug but also offers target release of drugs. SLN can be used as a carrier for lipophilic as well as hydrophilic drugs 4 . SLN provides stability to the solid lipid matrix and overcomes the disadvantages of liposomes, which includes stability problems 5 . Instead of polymeric nanoparticles, SLN are found to be more compatible with the biological system. Exclusive properties of SLN such as smaller size, larger surface area and interaction of phases at the interface make them valuable candidate 2 . The release of encapsulated compounds is controlled by solid lipid matrix, which also improves the stability of incorporated lipophilic ingredients. The type of lipids, surfactants and their concentration in the formulation of SLN adjust the particle size, drug loading, and release behavior of drugs 5 . The physicochemical characteristics of the solid lipid...

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Surface modification of solid lipid nanoparticles for oral delivery of curcumin: Improvement of bioavailability through enhanced cellular uptake, and lymphatic uptake

Cited by 170 publications

References 30 publications

Hepato therapeutic Efficacy of Native Curcumim and Nano –curcumin : A Novel Therapy Against Hyperthyroidism Induced Liver Oxidative and Inflammatory Damage in Rats

Hepato therapeutic Efficacy of Native Curcumim and Nano –curcumin : A Novel Therapy Against Hyperthyroidism Induced Liver Oxidative and Inflammatory Damage in Rats

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

Solid lipid nanoparticles: a promising technology for delivery of poorly water-soluble drugs

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