Lipid Carriers: A Versatile Delivery Vehicle for Proteins and Peptides

Rawat, Mamta; Singh, Deependra; Saraf, Swarnlata

doi:10.1248/yakushi.128.269

Cited by 103 publications

(65 citation statements)

References 70 publications

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“…However, the lipid matrix might be destroyed when the proportion of almond oil becomes excessive and the drug entrapment efficiency decreases. 11 Another advantage for Compritol ® 888 is that it could be a multifunction excipient, which is used as a lipid matrix for formation of the lipid particles, surfactant, and emulsifying agent. Furthermore, Compritol ® 888 decreases interfacial tension between the two phases leading to a homogeneous and stable emulsion, thus enhancing FLV entrapment in the FLV-NLC vesicles.…”

Section: Entrapment Efficiencymentioning

confidence: 99%

Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers

El-Helw¹,

Fahmy²

2015

IJN

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The aim of this study is to prepare fluvastatin nanostructured lipid carriers (FLV-NLCs) in order to find an innovative way to alleviate FLV-associated disadvantages. The limitations include poor solubility and extensive first-pass metabolism, resulting in low (30%) bioavailability and short elimination half-life (1–3 hours). FLV-NLCs were prepared by hot emulsification–ultrasonication method. Ten runs were created by three-level factorial design (3 2 ) to optimize FLV-NLCs formulation process. In this study, two factors, four responses, and three-level factorial design were endorsed. The studied variables were lipid:oil ratio ( X 1 ) and sonication time ( X 2 ). However, the responses parameter determined the particle size ( Y 1 , nm), entrapment efficiency percent (EE%, Y 2 ), particles zeta potential ( Y 3 ), and 80% of the drug release after 24 hours ( X 4 ). Furthermore, stability and in vivo pharmacokinetics were studied in rats. The optimized consisted formula had an average particle size of 165 nm with 75.32% entrapment efficiency and 85.32% of drug released after 24 hours, demonstrating a sustaining drug release over 24 hours. An in vivo pharmacokinetic study revealed enhanced bioavailability by >2.64-fold, and the mean residence time was longer than that of FLV. We concluded that NLCs could be promising carriers for sustained/prolonged FLV release with enhanced oral bioavailability.

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Section: Entrapment Efficiencymentioning

confidence: 99%

Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers

El-Helw¹,

Fahmy²

2015

IJN

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“…Of all the nanomaterials, lipid nanoparticles offer a number of advantages such as bioacceptable and biodegradable nature, making them less toxic as compared to other nanocarriers. 17,18 The NLCs are represented as an improved generation of lipid nanoparticles, which are developed from SLNs with improved characteristics. The general idea behind the system is to "mix solid lipid matrices with spatially incompatible liquid lipids, leading to imperfection in the structure of the lipid matrix", hence enhancing the drug-loading (DL) capacity.…”

mentioning

confidence: 99%

Acute and subacute toxicity profiles of thymoquinone-loaded nanostructured lipid carrier in BALB/c mice

Ong

Yazan

et al. 2016

IJN

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“…[11][12][13] SLN have been shown to have superior advantages over polymeric nanoparticles, fat emulsion and liposomes.…”

mentioning

confidence: 99%

“…10) The major excipients used in the development of the SLN are fatty acids, mono, di and triglycerides, phospholipids etc., which are part of the physiological composition and thus are biocompatible to the body. [11][12][13] SLN have been shown to have superior advantages over polymeric nanoparticles, fat emulsion and liposomes. 14) SLN can be produced on large scale and are also biocompatible to the body as compared to polymers, the monomeric unit of which are cytotoxic to the body.…”

mentioning

confidence: 99%

Formulation and Evaluation of Solid Lipid Nanoparticles of a Water Soluble Drug: Zidovudine

et al. 2010

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The drug delivery system using solid lipid nanoparticles (SLN) came into being about two decades ago and since then lot of work has been done in this field.1-5) SLN for oral drug administration are specifically used to target the uptake of the drug by lymphatic system which prevents its first pass metabolism. Lymphatic uptake of drugs follow two routes which include transcellular transport through the enterocyte and phagocytosis of the drugs by Mast cells of payer's patches lining the intestinal mucosa. [6][7][8] The production of this nano particulate system is based on the principle of solidification of lipid nano emulsion.9) The different technologies available for the fabrication of SLN are high shear homogenization, ultrasound, high pressure homogenization (cold homogenization and hot homogenization), solvent emulsification/evaporation and microemulsion method.10) The major excipients used in the development of the SLN are fatty acids, mono, di and triglycerides, phospholipids etc., which are part of the physiological composition and thus are biocompatible to the body. [11][12][13] SLN have been shown to have superior advantages over polymeric nanoparticles, fat emulsion and liposomes.14) SLN can be produced on large scale and are also biocompatible to the body as compared to polymers, the monomeric unit of which are cytotoxic to the body.15,16) SLN exhibit sustained release effect due to the immobility of drug within lipid as compared to the emulsion formulations 17) and also exhibit better physical and chemical stability of drug compared to liposome.18) This delivery system has been extensively used as carriers for proteins, protein drugs, vaccines and lipophilic water insoluble drugs. 19) SLN are potential delivery system for lipophilic drugs where aqueous solubility of the drug is the limiting factor for its absorption. [20][21][22] Moreover, the incorporation of such drugs within SLN is easier due to their affinity for the lipid. On the other hand, entrapment of hydrophilic drug inside the hydrophobic matrix of SLN is a real challenge as the drug has maximum tendency to partition in the water during the fabrication process. Although a few hydrophilic molecules have been incorporated into SLN like thymocratin, 23) insulin, 24) diminazene 25) and thymopentin, 26) lot more scope still remains for the entrapment of hydrophilic drugs into lipid nanoparticles.Zidovudine (AZT), a hydrophilic drug has been used in the present investigation. It belongs to the class of nucleoside reverse transcriptase inhibitor and is used in the treatment of AIDS. This drug has various disadvantages like short biological half life due to extensive first pass metabolism and dose related bone marrow toxicity. AZT is a potential candidate for delivery via lipid based nanoparticulate system as this would help to improve lymphatic uptake, avoid hepatic first pass metabolism and thus reduce the dose requirement and decrease the side effects. 27) Furthermore, sustained drug release would reduce dosing frequency and at the same time ma...

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Lipid Carriers: A Versatile Delivery Vehicle for Proteins and Peptides

Cited by 103 publications

References 70 publications

Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers

Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers

Acute and subacute toxicity profiles of thymoquinone-loaded nanostructured lipid carrier in BALB/c mice

Formulation and Evaluation of Solid Lipid Nanoparticles of a Water Soluble Drug: Zidovudine

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