Self-assembled lecithin-chitosan nanoparticles improve the oral bioavailability and alter the pharmacokinetics of raloxifene

Murthy, Aditya; Ravi, Punna Rao; Kathuria, Himanshu; Vats, Rahul

doi:10.1016/j.ijpharm.2020.119731

Cited by 43 publications

(27 citation statements)

References 63 publications

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“…Noticeably, all prepared NPs (unloaded) exhibited significant cationic surface charges, as shown in Table 3 , even under variable pH conditions (except for CSP-LC-TPP, which became slightly negative at pH 7.4, Table 3 ), indicating that their outer shells were composed mainly of cationic CS or CSP, while negatively charged LC remained mainly within NP cores. This conclusion is in parallel with previous reports (Chu et al, 2019 ; Jardim et al, 2020 ; Murthy et al, 2020 ).…”

Section: Resultssupporting

confidence: 92%

“…LC/CS-based NPs have been reported as successful in vitro and in vivo drug delivery vehicles (Sonvico et al, 2006 ; Chadha et al, 2012 ; Correa et al, 2020 ; Murthy et al, 2020 ). Moreover, CS-lecithin (LC, Figure 1 ) nanocomplex was also reported to be useful for the protection of siRNA in serum and subsequent cellular delivery (Sarmento et al, 2011 ; Trickler et al, 2011 ; Delgado et al, 2013 ).…”

Section: Introductionmentioning

confidence: 99%

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Novel Ellipsoid Chitosan-Phthalate Lecithin Nanoparticles for siRNA Delivery

Saeed

Abdullah

Ahram

et al. 2021

Front. Bioeng. Biotechnol.

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Section: Resultssupporting

confidence: 92%

Section: Introductionmentioning

confidence: 99%

Novel Ellipsoid Chitosan-Phthalate Lecithin Nanoparticles for siRNA Delivery

Saeed

Abdullah

Ahram

et al. 2021

Front. Bioeng. Biotechnol.

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“…Enhanced THQ bioavailability after oral administration THQ-CPLNPs was due to encapsulation of THQ into the small-sized particles that increase the solubility of THQ as well as the surface area that results in significantly higher absorption of THQ from GIT upon oral administration. Moreover, the mucoadhesive property of THQ-CPLNPs helps to increase residence time in GIT that leads to higher absorption, thereafter higher oral bioavailability of THQ (Murthy et al., 2020 ).…”

Section: Resultsmentioning

confidence: 99%

Thymoquinone-entrapped chitosan-modified nanoparticles: formulation optimization to preclinical bioavailability assessments

et al. 2021

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The major limitation with the oral administration of most of the phytochemicals is their low aqueous solubility and bioavailability. Thymoquinone (THQ) is one of the most widely used phytochemicals used to treat a variety of diseases. However, strong lipophilic characteristics limit its clinical application. Therefore, this study was aimed to design novel chitosan (C) modified polycaprolactone (PL) nanoparticles (NPs) for improved oral bioavailability of THQ. THQ-CPLNPs was optimized 33-Box–Behnken design. After that, the optimized THQ-CPLNPs was characterized by different parameters. THQ-CPLNPs showed the size, PDI, and ZP of 182.32 ± 6.46 nm, 0.179 ± 0.012, and +21.36 ± 1.22 mV, respectively. The entrapment and loading capacity were found to be 79.86 ± 4.36%, and 13.45 ± 1.38%, respectively. THQ-CPLNPs exhibited burst release in initial 2 h followed by prolonged release up to 24 h in simulated intestinal fluids. THQ-CPLNPs showed excellent mucoadhesion properties which were further confirmed with the intestinal permeation study as well as confocal microscopy. The study revealed higher permeation of THQ-CPLNPs compared to neat THQ suspension (THQ-S). Moreover, in vivo gastric irritation study revealed good compatibility of THQ-CPLNPs with the gastric mucosa. Furthermore, pharmacokinetic results depicted ∼3.53-fold improved oral bioavailability of THQ from THQ-CPLNPs than THQ-S. Therefore, from the findings, it was concluded that the prepared polymeric NPs could be an effective delivery system for improved oral bioavailability of THQ.

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“…Saini et al [26] developed intranasal RLX-loaded chitosan nanoparticles, which enhance RLX bioavailability by~1.7-fold. Murthy et al [22] developed soy lecithin-chitosan complex nanoparticles (LCNPs) for oral delivery of RLX. After loading RLX into LCNPs, its bioavailability increased significantly (p < 0.05) by over~4.2-fold compared to the free drug suspension.…”

Section: In Vivo Estimation Of Rlx Pharmacokinetics In Rabbitsmentioning

confidence: 99%

“…Different strategies have been made to improve RLX bioavailability: Murthy et al [22] developed Self-assembled lecithin-chitosan RLX nanoparticles, Shah et al [23] developed RLX nanostructured lipid carriers, Agardan et al [24] prepared RLX-loaded liposomes, Pandya et al [25] prepared an RLX nanoemulsion, and Saini et al [26] developed RLXloaded chitosan nanoparticles.…”

Section: Introductionmentioning

confidence: 99%

Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization

et al. 2021

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Green nanotechnology utilizes the principles of green chemistry to formulate eco-friendly nanocarrier systems to mitigate patients and environment hazards. Raloxifene (RLX) demonstrates poor aqueous solubility (BCS class II) and low bioavailability, only 2% (extensive first-pass metabolism). The aim of this study is to enhance RLX solubility and bioavailability via development of novel solid dispersed multilayered core-sheath RLX-loaded nanofibers (RLX-NFs) without the involvement of organic solvents. A modified emulsion electrospinning technique was developed. Electrospinning of an RLX-nanoemulsion (RLX-NE) with polymer solution (poly vinyl alcohol (PVA), hydroxypropyl methylcellulose (HPMC), and chitosan (CS) in different volume ratios (1:9, 2:8, and 4:6) using D-optimal response surface methodology was adopted. In vitro characterization of RLX-loaded NFs was performed; scanning electron microscope (SEM), thermal analysis, drug content, release studies, and bioadhesion potential. The optimum NFs formula was evaluated for morphology using high-resolution transmission electron microscopy (HRTEM), and ex vivo drug permeation. The superiority of E2 (comprising RLX-NE and PVA (2:8)) over other NF formulae was statistically observed with respect to Q60 (56.048%), Q240 (94.612%), fiber size (594.678 nm), mucoadhesion time 24 h, flux (5.51 µg/cm2/h), and enhancement ratio (2.12). RLX pharmacokinetics parameters were evaluated in rabbits following buccal application of NF formula E2, relative to RLX oral dispersion. E2 showed significantly higher Cmax (53.18 ± 4.56 ng/mL), and relative bioavailability (≈2.29-fold).

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Self-assembled lecithin-chitosan nanoparticles improve the oral bioavailability and alter the pharmacokinetics of raloxifene

Cited by 43 publications

References 63 publications

Novel Ellipsoid Chitosan-Phthalate Lecithin Nanoparticles for siRNA Delivery

Novel Ellipsoid Chitosan-Phthalate Lecithin Nanoparticles for siRNA Delivery

Thymoquinone-entrapped chitosan-modified nanoparticles: formulation optimization to preclinical bioavailability assessments

Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization

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