Nanostructured lipid (NLCs) carriers as a bioavailability enhancement tool for oral administration

Gaba, Bharti; Fazil, Mohammad; Ali, Asgar; Baboota, Sanjula; Sahni, Jasjeet Kaur; Ali, Javed

doi:10.3109/10717544.2014.898110

Cited by 123 publications

(48 citation statements)

References 61 publications

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“…After a 2-weeks treatment, the combination lowered cholesterol, glucose and triglycerides levels for extended periods and improved endothelial functioning (Ratnam et al, 2009). NLC are considered a potential bioavailability enhancement tool (Gaba et al, 2014). NLC of CoQ10 enhanced the aqueous dissolution and lowered the cytotoxicity as compared to a CoQ10 free suspension (Wang et al, 2012).…”

Section: Strategies For Maximizing Intracellular Deliverymentioning

confidence: 99%

Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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Coenzyme Q10 (CoQ10), also known as ubiquinone or ubidecarenone, is a powerful, endogenously produced, intracellularly existing lipophilic antioxidant. It combats reactive oxygen species (ROS) known to be responsible for a variety of human pathological conditions. Its target site is the inner mitochondrial membrane (IMM) of each cell. In case of deficiency and/or aging, CoQ10 oral supplementation is warranted. However, CoQ10 has low oral bioavailability due to its lipophilic nature, large molecular weight, regional differences in its gastrointestinal permeability and involvement of multitransporters. Intracellular delivery and mitochondrial target ability issues pose additional hurdles. To maximize CoQ10 delivery to its biopharmaceutical target, numerous approaches have been undertaken. The review summaries the current research on CoQ10 bioavailability and highlights the headways to obtain a satisfactory intracellular and targeted mitochondrial delivery. Unresolved questions and research gaps were identified to bring this promising natural product to the forefront of therapeutic agents for treatment of different pathologies.

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Section: Strategies For Maximizing Intracellular Deliverymentioning

confidence: 99%

Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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“…14 Solid lipid nanoparticles (SLNs) 15 and nanostructured lipid carriers 16 are the most widely used lipid vehicles. Due to involving no dissolution process, lipid nanocarriers theoretically can markedly enhance the oral absorption of BCS II drugs (eg, several or dozens of times increase in bioavailability); nevertheless, this is not always the case.…”

Section: Introductionmentioning

confidence: 99%

Effects of PEGylated lipid nanoparticles on the oral absorption of one BCS II drug: a mechanistic investigation

Zhang¹,

Chen²,

Zhang³

et al. 2014

IJN

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Lipid nanocarriers are becoming a versatile platform for oral delivery of lipophilic drugs. In this article, we aimed to explore the gastrointestinal behaviors of lipid nanoparticles and the effect of PEGylation on oral absorption of fenofibrate (FN), a Biopharmaceutics Classification System (BCS) II model drug. FN-loaded PEGylated lipid nanoparticles (FN-PLNs) were prepared by the solvent-diffusion method and characterized by particle size distribution, morphology, Fourier transform infrared spectroscopy, and drug release. Lipolytic experiments were performed to assess the resistance of lipid nanoparticles against pancreatic lipase. Pharmacokinetics was evaluated in rats after oral administration of FN preparations. The obtained FN-PLNs were 186.7 nm in size with an entrapment efficiency of >95%. Compared to conventional lipid nanoparticles, PLNs exhibited slower drug release in the lipase-containing medium, strikingly reduced mucin binding, and suppressed lipolysis in vitro. Further, oral absorption of FN was significantly enhanced using PLNs with relative bioavailability of 123.9% and 157.0% to conventional lipid nanoparticles and a commercial formulation (Lipanthyl ® ), respectively. It was demonstrated that reduced mucin trapping, suppressed lipolysis, and/or improved mucosal permeability were responsible for increased oral absorption. These results facilitated a better understanding of the in vivo fate of lipid nanoparticles, and suggested the potential of PLNs as oral carriers of BCS II drugs.

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“…[62,63] As the concentration of water-soluble surfactant will increase, the general HLB value of the NLC system also increases and this reduces the surface free energy of the dispersed phase, which ends up in decrease in particle size distribution of NLC system. Reduction in particle size distribution, more increase the general expanse of the mixture system and ultimately improves the entrapment efficiency.…”

Section: Effect Of Hydrophile-lipophile Balance (Hlb)mentioning

confidence: 99%

Comprehensive Interpretation of Nanostructured Lipid Carriers (Nlc): A Promising New Generation Lipid Carrier for the Delivery of Cancer Chemotherapeutics

Wang¹

2017

WJPR

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In the last couple of years, Nano-carries have attracted large amount of consideration in drug delivery specifically for cancer chemotherapy.There are shortcomings which greatly hindered anti-cancer drug delivery such as poor-aqueous solubility, toxicity towards normal tissues, limited targeting ability, inefficient large-scale production output, rapid degradation and quick release from the formulations. The amount of studies analyzing formulations based on nanostructured lipid carriers (NLCs) has been significantly increased. This increase in NLC investigation is possibly due to its ability to overcome the physiological obstacles and enhanced understanding of mechanism of action NLCs in vitro and in vivo via different route of administration in recent years. Toxicity related concerns like-presence of organic residues and polymers are tactically bypassed by using nanostructured lipid carriers. In this review we have discussed the types, preparation procedure and physicochemical characterization technique of NLCs. In addition, the roles NLCs can play in cancer

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Nanostructured lipid (NLCs) carriers as a bioavailability enhancement tool for oral administration

Abstract: On the basis of the literature survey done, it was concluded that the NLCs enhances the oral bioavailability of the drug and may decrease the side effects and toxicity of the lipids used in other polymeric NPs as NLCs uses physiological and biodegradable lipids.

Cited by 123 publications

References 61 publications

Strategies for oral delivery and mitochondrial targeting of CoQ10

Strategies for oral delivery and mitochondrial targeting of CoQ10

Effects of PEGylated lipid nanoparticles on the oral absorption of one BCS II drug: a mechanistic investigation

Comprehensive Interpretation of Nanostructured Lipid Carriers (Nlc): A Promising New Generation Lipid Carrier for the Delivery of Cancer Chemotherapeutics

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