Lipid nanocarrier of selegiline augmented anti-Parkinson’s effect via P-gp modulation using quercetin

Qamar, Zufika; Ashhar, Muhammad Usama; Annu, .; Qizilibash, Farheen Fatima; Sahoo, PK; Ali, Asgar; Ali, Javed; Baboota, Sanjula

doi:10.1016/j.ijpharm.2021.121131

Cited by 24 publications

(10 citation statements)

References 69 publications

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“…It was noted how much MG was getting dissolved in particular solid lipids. The production of a clean, transparent mixture served as proof of full disintegration ( Naseri et al, 2015 , Qamar et al, 2021 ). In the case of the selection of surfactant, lipophilicity was taken into consideration.…”

Section: Methodsmentioning

confidence: 99%

Preparation and evaluation of antidiabetic activity of mangiferin-loaded solid lipid nanoparticles

Foudah,

Ayman Salkini,

Alqarni

et al. 2024

Saudi Journal of Biological Sciences

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Section: Methodsmentioning

confidence: 99%

Preparation and evaluation of antidiabetic activity of mangiferin-loaded solid lipid nanoparticles

Foudah,

Ayman Salkini,

Alqarni

et al. 2024

Saudi Journal of Biological Sciences

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“…L-HA–PDM–INS–FITC, M-HA–PDM–INS–FITC, and H-HA–PDM–INS–FITC were prepared using the same method as for HA–PDM–INS. Briefly [ 43 ], the 0.2 mL of 5 IU/mL INS–FITC solution, L-HA–PDM–INS–FITC, M-HA–PDM–INS–FITC, and H-HA–PDM–INS–FITC were injected into the isolated intestine, and then the intestine was placed in 5 mL pH 7.4 PBS at 37 °C and 50 rpm stirring speed. At 1 and 2 h, the intestines were removed and rinsed separately.…”

Section: Methodsmentioning

confidence: 99%

pH-Responsive and Mucoadhesive Nanoparticles for Enhanced Oral Insulin Delivery: The Effect of Hyaluronic Acid with Different Molecular Weights

et al. 2023

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Drug degradation at low pH and rapid clearance from intestinal absorption sites are the main factors limiting the development of oral macromolecular delivery systems. Based on the pH responsiveness and mucosal adhesion of hyaluronic acid (HA) and poly[2-(dimethylamino)ethyl methacrylate] (PDM), we prepared three HA–PDM nano-delivery systems loaded with insulin (INS) using three different molecular weights (MW) of HA (L, M, H), respectively. The three types of nanoparticles (L/H/M-HA–PDM–INS) had uniform particle sizes and negatively charged surfaces. The optimal drug loadings of the L-HA–PDM–INS, M-HA–PDM–INS, H-HA–PDM–INS were 8.69 ± 0.94%, 9.11 ± 1.03%, and 10.61 ± 1.16% (w/w), respectively. The structural characteristics of HA–PDM–INS were determined using FT-IR, and the effect of the MW of HA on the properties of HA–PDM–INS was investigated. The release of INS from H-HA–PDM–INS was 22.01 ± 3.84% at pH 1.2 and 63.23 ± 4.10% at pH 7.4. The protective ability of HA–PDM–INS with different MW against INS was verified by circular dichroism spectroscopy and protease resistance experiments. H-HA–PDM–INS retained 45.67 ± 5.03% INS at pH 1.2 at 2 h. The biocompatibility of HA–PDM–INS, regardless of the MW of HA, was demonstrated using CCK-8 and live–dead cell staining. Compared with the INS solution, the transport efficiencies of L-HA–PDM–INS, M-HA–PDM–INS, and H-HA–PDM–INS increased 4.16, 3.81, and 3.10 times, respectively. In vivo pharmacodynamic and pharmacokinetic studies were performed in diabetic rats following oral administration. H-HA–PDM–INS exhibited an effective hypoglycemic effect over a long period, with relative bioavailability of 14.62%. In conclusion, these simple, environmentally friendly, pH-responsive, and mucoadhesive nanoparticles have the potential for industrial development. This study provides preliminary data support for oral INS delivery.

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“…The drug and liquid lipid blend were centrifuged, and the supernatants were taken out and solubilized with methanol. A UV spectrophotometer (UV1601 Instrument, Shimadzu, Japan) was used to determine the drug concentration in methanol at 311nm [21,22].…”

Section: Selection Of Lipidsmentioning

confidence: 99%

“…The sample was blended with KBr in a 1:50 (w/w) proportion for structural investigation by Fourier transform infrared FT-IR by Bruker. The mixture was prepared by triturating it in a mortar and pestle to form a super fine particle, which was then pressed into pellets by hydraulic pressure [22]. The pellets were used for chemical analysis of the sample by FT-IR spectroscopy.…”

Section: Chemical Analysis Of Lncs By Ft-ir Spectroscopymentioning

confidence: 99%

Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Muheem,

Wasim,

Aldosari

et al. 2023

Preprint

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Etravirine (ERVN) is a potential NNRTI (non-nucleoside reverse transcriptase inhibitor) in treating HIV infection. It possesses extremely low oral bioavailability. The present research aims to optimize the formulation and characterization of TPGS-enriched ERVN-loaded lipid-based nanocarriers (LNCs) for HIV-infected patients. The formulation, ERVN-TPGS-LNCs, was optimized by CCRD using a modified-solvent evaporation process. Various characterization parameters of LNCs were evaluated, including globule size of 121.56 ± 2.174 nm, PDI of 0.172 ± 0.042, the zeta potential of -7.32 ± 0.021 mV, %EE of 94.42 ± 8.65% of ETR and %DL was 8.94 ± 0.759% of ERVN and spherical shape was revealed by TEM. PXRD was also performed to identify the crystallinity of the sample. In-vitro drug release showed % a cumulative drug release of 79.77 ± 8.35% at pH 1.2 and 83.23 ± 9.11% at pH 6.8, respectively, at the end of 48h compared to pure drug suspension (ERVN-S). Further, the intestinal permeation study and confocal microscope showed approximately ~3-fold and ~2-fold increased permeation in ERVN-TPGS-LNCs and ERVN-LNCs across the gut sac compared to ERVN-S. Hemolysis compatibility and lipolysis studies were performed to predict the in-vivo fate of the formulation. The pharmacokinetic study revealed a 3.13-fold increment in the relative bioavailability, which agrees with the ex-vivo studies, and lymphatic uptake was validated by using cycloheximide (CYHD) along with designed formulation, which leads to lowering AUC of ERVN-TPGS-LNCs. Thus, this study ensures that ERVN-TPGS-LNCs take lymphatic uptake to minimize the first-pass metabolism followed by improved oral bioavailability of EVN. Thus, the enhanced bioavailability of ERVN can reduce the high dose of ERVN to minimize the adverse effects related to dose-related burden.

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Lipid nanocarrier of selegiline augmented anti-Parkinson’s effect via P-gp modulation using quercetin

Cited by 24 publications

References 69 publications

Preparation and evaluation of antidiabetic activity of mangiferin-loaded solid lipid nanoparticles

Preparation and evaluation of antidiabetic activity of mangiferin-loaded solid lipid nanoparticles

pH-Responsive and Mucoadhesive Nanoparticles for Enhanced Oral Insulin Delivery: The Effect of Hyaluronic Acid with Different Molecular Weights

Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

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