Self-assembled biodegradable polymeric micelles to improve dapoxetine delivery across the blood&amp;ndash;brain barrier

Abourehab, Mohammed A. S.; Ahmed, Osama A. A.; Balata, Gehan F.; Almalki, Waleed Hassan

doi:10.2147/ijn.s168148

Cited by 51 publications

(23 citation statements)

References 47 publications

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“…Dubey et al [43] demonstrated increased vesicle size of ethosomes with increasing PL content. In another study, Ahmed and Badr-Eldin [44] reported an increase in avanafil invasome size with increasing PL content of the vesicles. Regarding the HLB of the surfactant, it was observed that a significant reduction of the vesicle size occurs as the HLB is decreased.…”

Section: Discussionmentioning

confidence: 89%

RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

et al. 2020

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Flibanserin (FLB) is a nonhormonal medicine approved by the Food and Drug Administration (FDA) to treat the hypoactive sexual appetite disorder in females. However, the peroral administration of the medicine is greatly affected by its poor bioavailability as a result of its extensive first-pass effect and poor solubility. Aiming at circumventing these drawbacks, this work involves the formulation of optimized FLB transfersome (TRF) loaded intranasal hydrogel. Box–Behnken design was utilized for the improvement of FLB TRFs with decreased size. The FLB-to-phospholipid molar ratio, the edge activator hydrophilic lipophilic balance, and the pH of the hydration medium all exhibited significant effects on the TRF size. The optimized/developed TRFs were unilamellar in shape. Hydroxypropyl methyl cellulose based hydrogel filled with the optimized FLB TRFs exhibited an improved ex vivo permeation when compared with the control FLB-loaded hydrogel. In addition, the optimized TRF-loaded hydrogel exhibited higher bioavailability and enhanced brain delivery relative to the control hydrogel following intranasal administration in Wistar rats. The results foreshadow the possible potential application of the proposed intranasal optimized FLB-TRF-loaded hydrogel to increase the bioavailability and nose-to-brain delivery of the drug.

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Section: Discussionmentioning

confidence: 89%

RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

et al. 2020

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“…Poly(ethylene glycol)-b-poly(lactide-co-glycolide) (PEG-b-PGLA) seems to be a promising DDS [120][121][122], capable of passing the blood brain barrier [123,124]. Liu et al [125] investigated PEG 2000 / 5000 -b-PLGA (different ratio's) micelles on their biocompatibility and indicated that all micelles presented very low cytotoxicity.…”

Section: Peg-b-plgamentioning

confidence: 99%

Drug Delivery with Polymeric Nanocarriers—Cellular Uptake Mechanisms

Nelemans

Gurevich

2020

Materials

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Nanocarrier-based systems hold a promise to become “Dr. Ehrlich’s Magic Bullet” capable of delivering drugs, proteins and genetic materials intact to a specific location in an organism down to subcellular level. The key question, however, how a nanocarrier is internalized by cells and how its intracellular trafficking and the fate in the cell can be controlled remains yet to be answered. In this review we survey drug delivery systems based on various polymeric nanocarriers, their uptake mechanisms, as well as the experimental techniques and common pathway inhibitors applied for internalization studies. While energy-dependent endocytosis is observed as the main uptake pathway, the integrity of a drug-loaded nanocarrier upon its internalization appears to be a seldomly addressed problem that can drastically affect the uptake kinetics and toxicity of the system in vitro and in vivo.

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“…The prepared VNP-TPGS-ALA dispersion was investigated for mean particle size by light scattering technique using a Zetatrac particle size analyzer (Microtrac Inc., Montgomeryville, PA, USA). 28…”

Section: Evaluation Of Vnp-tpgs-ala Micelles Particle Sizementioning

confidence: 99%

Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies

Ahmed¹,

El-Say²,

Aljaeid³

et al. 2018

IJN

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BackgroundVinpocetine (VNP), a semisynthetic natural product, is used as a vasodilator for cerebrovascular and age-related memory disorders. VNP suffers from low oral bioavailability owing to its low water solubility and extensive first-pass metabolism. This work aimed at utilizing D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and alpha lipoic acid (ALA) to develop efficient micellar system for transdermal delivery of VNP.Materials and methodsVNP-TPGS-ALA micelles were prepared, characterized for particle size using particle size analyzer, and investigated for structure using transmission electron microscope. Optimization of VNP-TPGS-ALA micelles-loaded transdermal films was performed using Box–Behnken experimental design. The investigated factors were percentage of ALA in TPGS (X1), citral concentration (X2), and propylene glycol concentration (X3). Elongation percent (Y1), initial permeation after 2 hours (Y2), and cumulative permeation after 24 hours (Y3) were studied as responses.ResultsStatistical analysis revealed optimum levels of 16.62%, 3%, and 2.18% for X1, X2, and X3, respectively. Fluorescent laser microscopic visualization of skin penetration of the optimized transdermal film revealed marked widespread fluorescence intensity in skin tissue after 0.5, 2, and 4 hours compared with raw VNP transdermal film formulation, which indicated enhancement of VNP skin penetration.ConclusionThe obtained results highlighted the potentiality of VNP nanostructure-based films for controlling the transdermal permeation of the drug and improving its effectiveness.

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Self-assembled biodegradable polymeric micelles to improve dapoxetine delivery across the blood–brain barrier

Cited by 51 publications

References 47 publications

RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

Drug Delivery with Polymeric Nanocarriers—Cellular Uptake Mechanisms

Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies

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Self-assembled biodegradable polymeric micelles to improve dapoxetine delivery across the blood&ndash;brain barrier

Cited by 51 publications

References 47 publications

RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

RETRACTED: Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

Drug Delivery with Polymeric Nanocarriers—Cellular Uptake Mechanisms

Optimized vinpocetine-loaded vitamin E D-&alpha;-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies

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Product

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Self-assembled biodegradable polymeric micelles to improve dapoxetine delivery across the blood–brain barrier

Optimized vinpocetine-loaded vitamin E D-α-tocopherol polyethylene glycol 1000 succinate-alpha lipoic acid micelles as a potential transdermal drug delivery system: in vitro and ex vivo studies