Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride

Ranpise, Nisharani S.; Korabu, Swati S.; Ghodake, Vinod

doi:10.1016/j.colsurfb.2013.12.012

Cited by 73 publications

(38 citation statements)

References 20 publications

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“…In addition to selecting best lipid on the basis of solubility, compatibility studies between lipid and drug are also necessary to produce stable NLCs. Phase separation has been reported for various combinations of solid and liquid lipids and the combinations showing no separation till 24 h after mixing are selected for formulating stable NLCs [55]. Hydrophilic drugs have also been successfully entrapped in lipids, for example montelukast showed high entrapment efficiency (96.13%) with lipids, in other words, Precirol ATO 5 and Caproyl 90 in which it had highest solubility [53].…”

Section: Fabrication Of Nlcsmentioning

confidence: 99%

“…Ranpise et al . observed that smaller particle size with a high entrapment efficiency was obtained using a solvent evaporation method whereas ultrasonification method yielded higher sized particles with a low-encapsulation efficiency [55]. Furthermore, improved entrapment efficiency has been obtained using the melt-emulsification technique instead of solvent-diffusion method as solubility of drug in the aqueous phase is promoted during the diffusion of organic solvent in later method, which leads to decreased encapsulation of drug and is found to be more accumulated on the surface of NLCs [20].…”

Section: Fabrication Of Nlcsmentioning

confidence: 99%

“…Various mechanisms have been proposed for NLCs disposition inside the body either via their selective uptake through lacteals or payer's patches [55,69–70]. As drug-loaded NLCs pass consecutively through the digestive system, they undergo lipid digestion process step by step.…”

Section: Mechanism Of Nlcs Dispositionmentioning

confidence: 99%

See 2 more Smart Citations

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Poonia¹,

Kharb

Lather³

et al. 2016

Future Sci. OA

146

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Oral delivery is the most accepted and economical route for drug administration and leads to substantial reduction in dosing frequency. However, this route still remains a challenge for the pharmaceutical industry due to poorly soluble and permeable drugs leading to poor oral bioavailability. Incorporating bioactives into nanostructured lipid carriers (NLCs) has helped in boosting their therapeutic functionality and prolonged release from these carrier systems thus providing improved pharmacokinetic parameters. The present review provides an overview of noteworthy studies reporting impending benefits of NLCs in oral delivery and highlights recent advancements for developing engineered NLCs either by conjugating polymers over their surface or modifying their charge to overcome the mucosal barrier of GI tract for active transport across intestinal membrane.

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Section: Fabrication Of Nlcsmentioning

confidence: 99%

Section: Fabrication Of Nlcsmentioning

confidence: 99%

See 1 more Smart Citation

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Poonia¹,

Kharb

Lather³

et al. 2016

Future Sci. OA

146

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“…The transport study of CAR-NLCs versus CAR-S was performed as per the reported method using diffusion cell having area of 1.4 cm 2 (Liu et al, 2011;Ranpise et al, 2014). The study was performed using phosphate buffer:PEG400 at pH 7.4 (7:3) as the receptor media.…”

Section: Ex Vivo Transport Studymentioning

confidence: 99%

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

et al. 2016

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The purpose of this study was to develop Carvedilol nanostructured lipid carriers (CAR-NLCs) using stearic acid and oleic acid as lipid, and to estimate the potential as oral delivery system for poorly water soluble drug. The particle-size analysis revealed that all the developed formulations were within the nanometer range. The EE and loading were found to be between 69.45-88.56% and 9.58-12.56%, respectively. The CAR-NLCopt showed spherical morphology with smooth surface under transmission electron microscope (TEM). The crystallization of the drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC) and revealed that the drug was in an amorphous state in the NLC matrix. The ex vivo gut permeation study showed many folds increment in the permeation of CAR-NLCs compared to Carvedilol suspension (CAR-S). The oral bioavailability study of CAR was carried out using Wistar rats and relative bioavailability of CAR-NLCopt was found to be 3.95 fold increased in comparison with CAR-S. In vivo antihypertensive study in Wistar rats showed significant reduction in mean systolic BP by CAR-NLCopt vis-à-vis CAR-S (p50.05) owing to the drug absorption through lymphatic pathways. In conclusion, the NLC formulation remarkably improved the oral bioavailability of CAR and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs. The promising findings in this investigation suggest the practicability of these systems for the enhancement of bioavailability of CAR.

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“…Nevertheless, in oral drug delivery there is a need for innovative drug delivery systems due to low drug solubility, poor gastrointestinal absorption, metabolism related variability issues, continuous fluctuation of drug plasma levels and food effects [7,8]. Nebivolol is absorbed rapidly after oral administration and is not affected by food; however, it has variable absolute oral bioavailability due to its extensive first-pass metabolism [9].…”

Section: Introductionmentioning

confidence: 99%

Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet

Gökçe¹,

Kaynak²,

Yurdasiper³

et al. 2018

jrp

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ABSTRACT:The oral application of drugs is the most popular route for achieving systemic effects, nevertheless, it is limited by difficulties related to physicochemical properties of the drug. Solid lipid nanoparticles (SLNs) are appealing extensive notice because of showing increased solubility and improved oral bioavailability via different mechanisms. The aim of the study is to compare and peruse the in-situ permeation of nebivolol (NBV) loaded SLN and its commercial tablet formulation used for the treatment of hypertension. For this aim Single-Pass Intestinal Perfusion (SPIP) method was used for in-situ permeation studies. NBV loaded SLNs were prepared and modified with polyethylene glycol (PEG). In order to prepare SLNs by homogenization technique, compritol, lecithin and poloxamer were chosen. Particle sizes of blank and loaded SLN were 213.4±17.5 and 264.1±18.8 nm, respectively with polydispersity index values of approximately 0.3 for each. NBV loading resulted in positive electrical charge on SLNs. The encapsulation efficiency was 98.04±0.2 %. Permeability coefficient values were tripled when NBV was incorporated in SLNs and doubled when pure NBV was given separately with a blank SLN. PEG modified SLN can be used to enhance oral absorption of NBV, and SLNs alone can be used as permeation enhancer in oral drug delivery..

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Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride

Cited by 73 publications

References 20 publications

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet

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