Solid lipid nanoparticles for oral drug delivery: Chitosan coating improves stability, controlled delivery, mucoadhesion and cellular uptake

Luo, Yangchao; Teng, Zi; Li, Ying; Wang, Qin

doi:10.1016/j.carbpol.2014.12.084

Cited by 284 publications

(130 citation statements)

References 38 publications

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“…4,[173][174][175] Chitosan has various advantages over other polymers including lower toxicity, enhanced absorption and high mucoadhesive and antimicrobial properties which enhance the oral delivery of the phyto-bioactive compounds. In order to further enhance the absorption properties of the chitosan-coated SLNs, grafting of chitosan moieties was done through conjugation of amine and hydroxyl groups leading to functional chitosan like TMC.…”

Section: Chitosan-based Surface Modification Of Sln Delivery Systems mentioning

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

135

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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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Section: Chitosan-based Surface Modification Of Sln Delivery Systems mentioning

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

135

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“…To improve the oral absorption and bioavailability of poorly water-soluble drugs, many nanocarriers like SLN and NLC are used extensively. [75][76][77] NLC has gained attention because of biocompatibility, physicochemical stability, and ease of production. 78 NLCs are known to improve the transportation of drug through the intestinal epithelial layer and render protection against the vicious environment of gastrointestinal tracts.…”

mentioning

confidence: 99%

Inhibitory effect of a new orally active cedrol-loaded nanostructured lipid carrier on compound 48/80-induced mast cell degranulation and anaphylactic shock in mice

Chakraborty¹,

Kar²,

Kumari³

et al. 2017

IJN

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Background Type I hypersensitivity is an allergic reaction characterized by the overactivity of the immune system provoked by normally harmless substances. Glucocorticoids, anti-histamines, or mast cell stabilizers are the choices of treatment for type I hypersensitivity. Even though these drugs have the anti-allergic effect, they can have several side effects in prolong use. Cedrol is the main bioactive compound of Cedrus atlantica with anti-tumor, anti-oxidative, and platelet-activating factor inhibiting properties. Methods In this study, the preparation and anti-anaphylactic effect of cedrol-loaded nanostructured lipid carriers (NLCs) were evaluated. NLCs were prepared using Compritol ® 888 ATO and triolein as lipid phase and vitamin E d -α-tocopherylpolyethyleneglycol 1000 succinate, soya lecithin, and sodium deoxycholate as nanoparticle stabilizers. Results The average diameter of cedrol-NLCs (CR-NLCs) was 71.2 nm (NLC-C 1 ) and 91.93 nm (NLC-C 2 ). The particle had negative zeta potential values of −31.9 mV (NLC-C 1 ) and −44.5 mV (NLC-C 2 ). Type I anaphylactoid reaction in the animal model is significantly reduced by cedrol and cedrol-NLC. This in vivo activity of cedrol resulted that cedrol suppressed compound 48/80-induced peritoneal mast cell degranulation and histamine release from mast cells. Furthermore, compound 48/80-evoked Ca 2+ uptake into mast cells was reduced in a dose-dependent manner by cedrol and cedrol-NLC. Studies confirmed that the inhibition of type I anaphylactoid response in vivo in mice and compound 48/80-induced mast cell activation in vitro are greatly enhanced by the loading of cedrol into the NLCs. The safety of cedrol and CR-NLC was evaluated as selectivity index (SI) with prednisolone and cromolyn sodium as positive control. SI of CR-NLC-C 2 was found to be 11.5-fold greater than both prednisolone and cromolyn sodium. Conclusion Administration of CR-NLC 24 hours before the onset of anaphylaxis can prevent an anaphylactoid reaction. NLCs could be a promising vehicle for the oral delivery of cedrol to protect anaphylactic reactions.

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“…32 The substantial increase in PDI value for a higher S100-TCA level (100 mg) was attributed to the excess S100-TCA that failed to get completely adsorbed on to the NLCs and could have assembled into the small sized, thus leading to the increased PDI value. 33 The localization of PEG over the NLC surfaces could have resulted in increased ζ-potential of NLCs, 34 as reduced surface negativity of the nanocarrier on modification with different amounts of S100-TCA is evident from Table 1. It has been reported that -20 to -11 mV surface charge might not provide sufficient stability to the dispersions.…”

Section: Results and Discussion S100-tca Synthesis And Characterizationmentioning

confidence: 99%

Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

Tian¹,

Asghar²,

Wu³

et al. 2017

IJN

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The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (−7 to −3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs.

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Solid lipid nanoparticles for oral drug delivery: Chitosan coating improves stability, controlled delivery, mucoadhesion and cellular uptake

Cited by 284 publications

References 38 publications

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

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

Inhibitory effect of a new orally active cedrol-loaded nanostructured lipid carrier on compound 48/80-induced mast cell degranulation and anaphylactic shock in mice

Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

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