Augmented Oral Bioavailability and Prokinetic Activity of Levosulpiride Delivered in Nanostructured Lipid Carriers

Arif, Sadia Tabassam; Zaman, Shahiq uz; Khan, Muhammad Ayub; Tabish, Tanveer A.; Sohail, Muhammad; Arshad, Rabia; Kim, Jin‐Ki; Zeb, Alam

doi:10.3390/pharmaceutics14112347

Cited by 5 publications

(3 citation statements)

References 55 publications

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“…The composition of the optimized formulation was 80.55% Precirol ®® ATO 5, 19.45% Labrasol and 5% Tween 80/Span 80 mixture. The detailed results of the preliminary study have been described in Sadia et al [ 29 ].…”

Section: Methodsmentioning

confidence: 99%

Enhanced Antidepressant Activity of Nanostructured Lipid Carriers Containing Levosulpiride in Behavioral Despair Tests in Mice

Arif,

Khan,

Zaman

et al. 2023

Pharmaceuticals

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The potential of levosulpiride-loaded nanostructured lipid carriers (LSP-NLCs) for enhanced antidepressant and anxiolytic effects was evaluated in the current study. A forced swim test (FST) and tail suspension test (TST) were carried out to determine the antidepressant effect whereas anxiolytic activity was investigated using light–dark box and open field tests. Behavioral changes were evaluated in lipopolysaccharide-induced depressed animals. The access of LSP to the brain to produce therapeutic effects was estimated qualitatively by using fluorescently labeled LSP-NLCs. The distribution of LSP-NLCs was analyzed using ex vivo imaging of major organs after oral and intraperitoneal administration. Acute toxicity studies were carried out to assess the safety of LSP-NLCs in vivo. An improved antidepressant effect of LSP-NLCs on LPS-induced depression showed an increase in swimming time (237 ± 51 s) and struggling time (226 ± 15 s) with a reduction in floating (123 ± 51 s) and immobility time (134 ± 15 s) in FST and TST. The anxiolytic activity in the light–dark box and open field tests exhibited superiority over LSP dispersion. Near-infrared images of fluorescently labeled LSP-NLCs demonstrated the presence of coumarin dye in the brain after 1 h of administration. An acute toxicity study revealed no significant changes in organ-to-body weight ratio, serum biochemistry or tissue histology of major organs. It can be concluded that nanostructured lipid carriers can efficiently deliver LSP to the brain for improved therapeutic efficacy.

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Section: Methodsmentioning

confidence: 99%

Enhanced Antidepressant Activity of Nanostructured Lipid Carriers Containing Levosulpiride in Behavioral Despair Tests in Mice

Arif,

Khan,

Zaman

et al. 2023

Pharmaceuticals

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“…In vivo pharmacokinetic study 4.38-fold improvement in oral bioavailability of LSP than drug dispersion [132] Amisulpride (AMS)…”

Section: Dyspepsiamentioning

confidence: 99%

Nanostructured Lipid Carriers for Improved Delivery of Therapeutics via the Oral Route

Mahor,

Singh,

Gupta

et al. 2023

Journal of Nanotechnology

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Drug delivery via the oral route has always been challenging for poorly soluble drugs. Acid-induced hydrolysis, enzymatic degradation, and poor mucosal absorbency remain the primary hiccups for effective oral delivery of medications. With the advent of nanotechnology, nanostructured lipid carriers (NLCs) have emerged as a promising delivery carrier that can circumvent gastrointestinal tract (GIT) barriers hindering the solubility and bioavailability of such drugs. These NLCs can efficiently transport drug moieties across intestinal membranes shielding medications from intestinal pH and enzymatic degradation. Because they are composed of lipidic materials, they can be easily absorbed or taken up by various pathways such as transcellular absorption, paracellular transport, and M-cell uptake. Such mechanisms not only improve the absorption and solubility of drugs but also augment bioavailability and residence time and may bypass first-pass metabolism. This review explores the diverse applications of nanostructured lipid carriers (NLCs) in oral drug delivery for various medical conditions, shedding light on their current regulatory status, including FDA-approved options and those in pre/clinical stages. The review also features patented NLC formulations. It provides valuable insights into how NLCs can be harnessed for effective oral drug delivery and outlines recent advancements in optimizing their performance to tackle gastrointestinal barriers, thus opening new possibilities for NLCs in future pharmaceutical applications.

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“…The selection of AO or BO as the liquid lipid component of NLCs is based on several factors: their natural origin, compatibility with the skin's lipophilic constituents, capacity to improve drug penetration, and ability to provide a moisturizing effect [23]. In order to achieve increased physical stability of nanoparticulate dispersions, a mixture of the biocompatible PSMO and SMO was used [24,25].…”

Section: Introductionmentioning

confidence: 99%

Bigel Formulations of Nanoencapsulated St. John’s Wort Extract—An Approach for Enhanced Wound Healing

Sotirova

Gugleva

Stoeva

et al. 2023

Gels

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This study aimed to develop a semisolid vehicle for topical delivery of nanoencapsulated St. John’s wort (SJW) extract, rich in hyperforin (HP), and explore its wound-healing potential. Four nanostructured lipid carriers (NLCs) were obtained: blank and HP-rich SJW extract-loaded (HP-NLC). They comprised glyceryl behenate (GB) as a solid lipid, almond oil (AO), or borage oil (BO) representing the liquid lipid, along with polyoxyethylene (20) sorbitan monooleate (PSMO) and sorbitan monooleate (SMO) as surfactants. The dispersions demonstrated anisometric nanoscale particles with acceptable size distribution and disrupted crystalline structure, providing entrapment capacity higher than 70%. The carrier exhibiting preferable characteristics (HP-NLC2) was gelled with Poloxamer 407 (PM407) to serve as the hydrophilic phase of a bigel, to which the combination of BO and sorbitan monostearate (SMS) organogel was added. The eight prepared bigels with different proportions (blank and nanodispersion-loaded) were characterized rheologically and texturally to investigate the impact of the hydrogel-to-oleogel ratio. The therapeutic potential of the superior formulation (HP-NLC-BG2) was evaluated in vivo on Wistar male rats through the tensile strength test on a primary-closed incised wound. Compared with a commercial herbal semisolid and a control group, the highest tear resistance (7.764 ± 0.13 N) was achieved by HP-NLC-BG2, proving its outstanding wound-healing effect.

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Augmented Oral Bioavailability and Prokinetic Activity of Levosulpiride Delivered in Nanostructured Lipid Carriers

Cited by 5 publications

References 55 publications

Enhanced Antidepressant Activity of Nanostructured Lipid Carriers Containing Levosulpiride in Behavioral Despair Tests in Mice

Enhanced Antidepressant Activity of Nanostructured Lipid Carriers Containing Levosulpiride in Behavioral Despair Tests in Mice

Nanostructured Lipid Carriers for Improved Delivery of Therapeutics via the Oral Route

Bigel Formulations of Nanoencapsulated St. John’s Wort Extract—An Approach for Enhanced Wound Healing

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