Solidified nanostructured lipid carrier (S-NLC) for enhancing the oral bioavailability of ezetimibe

Shevalkar, Ganesh B.; Vavia, Pradeep R.

doi:10.1016/j.jddst.2019.101211

Cited by 26 publications

(19 citation statements)

References 47 publications

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“… In rats, bioavailability of atorvastatin loade NLCs revealed 3.6- and 2.1-fold increase in bioavailability when compared to atorvastatin suspension and commercial product (Lipitor ™) ( Elmowafy et al 2017 ), Ezetimibe Monosteol™ (solid lipid), Capryol™ 90 (liquid lipid), Kolliphor® EL (surfactant) and Transcutol® HP (Cosurfactant). In rats, bioavailability of ezetimibe loaded NLCs revealed 2.5- and 1.6-fold increase in bioavailability when compared to atorvastatin suspension and commercial product (Lipitor ™) ( Shevalkar and Vavia 2019 ). Amisulpride Gelucire®43/01(solid lipid), Capryol™90 (liquid lipid) and Tween-80 (surfactant) The relative bioavailability of NLCs capsules was found to be 252.78% when compared to Amipride® tablets ( Assasy et al, 2019 ).…”

Section: Applications Of Nlcsmentioning

confidence: 99%

Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies

Elmowafy

Al‐Sanea

2021

Saudi Pharmaceutical Journal

136

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NLCs have provoked the incessant impulsion for the development of safe and valuable drug delivery systems owing to their exceptional physicochemical and then biocompatible characteristics. Throughout the earlier period, a lot of studies recounting NLCs based formulations have been noticeably increased. They are binary system which contains both solid and liquid lipids aiming to produce less ordered lipidic core. Their constituents particularly influence the physicochemical properties and effectiveness of the final product. NLCs can be fabricated by different techniques which are classified according to consumed energy. More utilization NLCs is essential due to overcome barriers surrounded by the technological procedure of lipid-based nanocarriers’ formulation and increased information of the core mechanisms of their transport via various routes of administration. They can be used in different applications and by different routes such as oral, cutaneous, ocular and pulmonary. This review article seeks to present an overview on the existing situation of the art of NLCs for future clinics through exposition of their applications which shall foster their lucid use. The reported records evidently demonstrate the promise of NLCs for innovate therapeutic applications in the future.

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Section: Applications Of Nlcsmentioning

confidence: 99%

Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies

Elmowafy

Al‐Sanea

2021

Saudi Pharmaceutical Journal

136

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“…Keeping in mind the lipophilic nature of CIC and its poor water solubility with log p value of 5.3, one can understand the highest CIC payload with maximum solubility in precirol (327.01 µg/ml) followed by compritol (293.96 µg/ml) as predicted from Figure 2 . Although both of them are lipophilic triglycerides of long chain fatty acids (C18 and C22, respectively) with absence of PEG esters and low HLB value of ∼2 (Hamdani et al., 2003 ), the superior solubility of precirol stem from the difference in their crystalline properties where, the low tendency of precirol to crystallize into different polymorphic forms host more CIC (Shevalkar & Vavia, 2019 ) in contrast to highly crystalline compritol with perfect lattice (Huang et al., 2008 ).…”

Section: Resultsmentioning

confidence: 99%

“…The solubility of CIC in solid lipids was examined visually for the presence or absence of drug crystals. The maximum amount of the drug that remained soluble and beyond which precipitation took place was regarded as the solubility of the drug (Shevalkar & Vavia, 2019 ). Solubility in liquid lipid was estimated after separating the undissolved CIC by centrifugation at 15,000 rpm, at 25 °C for 20 min and the supernatant was separated and diluted with methanol.…”

Section: Methodsmentioning

confidence: 99%

Enhanced alveo pulmonary deposition of nebulized ciclesonide for attenuating airways inflammations: a strategy to overcome metered dose inhaler drawbacks

et al. 2021

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Ciclesonide (CIC), an inhaled corticosteroid for bronchial asthma is currently available as metered dose inhaler (CIC-MDI) which possesses a major challenge in the management of the elderly, critically ill patients and children. In this work, nebulized CIC nano-structure lipid particles (CIC-NLPs) were prepared and evaluated for their deep pulmonary delivery and cytotoxicity to provide additional clinical benefits to patients in controlled manner and lower dose. The bio-efficacy following nebulization in ovalbumin (OVA) induced asthma Balb/c mice compared to commercial (CIC-MDI) was also assessed. The developed NLPs of 222.6 nm successfully entrapped CIC (entrapment efficiency 93.3%) and exhibited favorable aerosolization efficiency (mass median aerodynamic diameter (MMAD) 2.03 lm and fine particle fraction (FPF) of 84.51%) at lower impactor stages indicating deep lung deposition without imparting any cytotoxic effect up to a concentration of 100 lg/ml. The nebulization of 40 mg dose of the developed CIC-NLPs revealed significant therapeutic impact in the mitigation of the allergic airways inflammations when compared to 80 mg dose of the commercial CIC-MDI inhaler (Alvesco V R ). Superior anti-inflammatory and antioxidative stress effects characterized by significant decrease (p< .0001) in inflammatory cytokines IL-4 and 13, serum IgE levels, malondialdehyde (MDA), nitric oxide (NO), TNF-a, and activated nuclear factor-jB (NF-jB) activity were obvious with concomitant increase in superoxide dismutase (SOD) activity. Histological examination with inhibition of inflammatory cell infiltration in the respiratory tract was correlated well with observed biochemical improvement.

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“…The same strategy has been used with other statins to improve their bioavailability through enhancing lymphatic uptake, such as simvastatin [ 106 ], rosuvastatin [ 107 ], and fluvastatin [ 108 ], as well as other agents, such as fibrates [ 109 , 110 , 111 ] and the cholesterol absorption inhibitor ezetimibe [ 112 , 113 , 114 ].…”

Section: Treating Cvd Through Various Administration Routesmentioning

confidence: 99%

Focus on the Lymphatic Route to Optimize Drug Delivery in Cardiovascular Medicine

et al. 2021

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While oral agents have been the gold standard for cardiovascular disease therapy, the new generation of treatments is switching to other administration options that offer reduced dosing frequency and more efficacy. The lymphatic network is a unidirectional and low-pressure vascular system that is responsible for the absorption of interstitial fluids, molecules, and cells from the peripheral tissue, including the skin and the intestines. Targeting the lymphatic route for drug delivery employing traditional or new technologies and drug formulations is exponentially gaining attention in the quest to avoid the hepatic first-pass effect. The present review will give an overview of the current knowledge on the involvement of the lymphatic vessels in drug delivery in the context of cardiovascular disease.

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Solidified nanostructured lipid carrier (S-NLC) for enhancing the oral bioavailability of ezetimibe

Cited by 26 publications

References 47 publications

Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies

Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies

Enhanced alveo pulmonary deposition of nebulized ciclesonide for attenuating airways inflammations: a strategy to overcome metered dose inhaler drawbacks

Focus on the Lymphatic Route to Optimize Drug Delivery in Cardiovascular Medicine

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