Design of long acting invasomal nanovesicles for improved transdermal permeation and bioavailability of asenapine maleate for the chronic treatment of schizophrenia

El-Tokhy, Fatma Sa’eed; Abdel-Mottaleb, Mona M.A.; El-Ghany, Elsayed A.; Geneidi, Ahmed S.

doi:10.1016/j.ijpharm.2021.121080

Cited by 22 publications

(13 citation statements)

References 30 publications

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“…Previous works have studied the transdermal delivery of ASP via invasomes. Invasomes are soft vesicular nanosystems that are prepared using natural terpenes as penetration enhancers for enhancing drug permeation through the skin [ 41 ]. The pharmacokinetics of two types of lipidic nanoparticles—nanocapsules and nanovesicles—were compared.…”

Section: Resultsmentioning

confidence: 99%

Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia

et al. 2023

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Lipid nanocapsules (LNCs) are promising for transdermal drug delivery due to their higher permeability-enhancing effects compared to polymeric nanoparticles. Lavender oil is an essential oil consisting of several terpenes (primarily linalool and linalyl acetate) known for their profound permeation-enhancing action. In the present work, we successfully encapsulated asenapine maleate (a second-generation antipsychotic that is highly metabolized by the liver, reducing its oral bioavailability) into biocompatible LNCs for transdermal application using a novel oily phase, i.e., lavender oil (LO-LNCs). A comparative study was conducted to determine the effects of different oily phases (i.e., Miglyol® 812, Labrafil® M1944CS, and Labrafac™ PG) on the LNCs. Surfactant types (Kolliphor® HS15, Kolliphor® EL and Tween80) and oil:surfactant ratios were studied. Blank and asenapine-loaded LNCs were optimized for particle size, polydispersity index, zeta potential, drug content and ex vivo skin permeation. Lavender oil and Labrafil® showed smaller vesicular sizes, while LO-LNCs increased the permeation of ASP across rat skin. In vivo pharmacokinetics revealed that LO-LNCs could increase the ASP Cmax via transdermal application by fourfold compared to oral suspension. They increased the bioavailability of ASP by up to 52% and provided sustained release for three days. The pharmacokinetic profile of the LO-LNCs was compared to ASP-loaded invasomes (discussed in a previous study) to emphasize LNCs’ transdermal delivery behavior.

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Section: Resultsmentioning

confidence: 99%

Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia

et al. 2023

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“…All findings were recorded as mean ± standard deviation. Study of one-way variance followed by a post-hoc test (Tukey 's test) using GraphPad ® Instat software version 3.06 (GraphPad Software, Inc., La Jolla, CA) was carried out for multiple comparison (n= 3), and statistical significance was described as P< 0.05 33 .…”

Section: Discussionmentioning

confidence: 99%

Chitosan Based Polyelectrolyte Complex Nanoparticles: Preparation and Characterization

Abuelella

Abd-Allah²,

Soliman³

et al. 2022

Bulletin of Pharmaceutical Sciences. Assiut

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Recently, the use of biodegradable polymers for specialized applications such as controlled release of drug formulations gained considerable attention. Biodegradable nanoparticles have been widely utilized in drug delivery systems. In this work polyelectrolyte complexation was used to prepare chitosan nanoparticles. The preparation process and major parameters were discussed and optimized. The nanoparticles were prepared by the polyelectrolyte complexation of chitosan (CS) with hyaluronate (HA). Studies were performed to identify effect of chitosan and hyaluronate molecular weight, chitosan: hyaluronate mass ratio and the effects of the aqueous chitosan solution pH on the particle size of nanoparticles. Nanoparticles were characterized by particle size analysis, polydispersity index, zeta potential and transmission electron microscope (TEM). Results showed that nanoparticles could be prepared only within an optimal zone of appropriate chitosan and hyaluronate molecular weights and CS:HA mass ratio. Increasing the hyaluronate molecular weight from low to high led to a significant enlargement in the particle size of the prepared nanoparticles with different chitosan molecular weights. Besides, we found that increasing the hyaluronate content at mass ratio 1:2 of CS:HA led to precipitation of nanoparticles . The particle sizes of the chitosan/HA nanoparticles significantly decreased with the increase of chitosan solution pH. The spherical shaped chitosan/HA nanoparticles were confirmed by TEM. The study showed that systematic design and modulation of the particle size of chitosan/HA polyelectrolyte complexes can be readily achieved with right control of critical processing parameters.

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“…Liposomes are vesicular systems containing phospholipids [26]. Other vesicular carriers have been developed over the years including ethosomes [11,27], invasomes [28,29], transfersomes [11] and bilosomes [30], and they all have other ingredients than phospholipids [25,26]. For instance, in bilosomes, there are bile salts [30].…”

Section: Nanocarriers Bearing Citrus Oils or Citrus Terpenesmentioning

confidence: 99%

“…Concerning nanometric systems intended for skin application, both a localized effect on the skin [11,31,34,36,37] or a systemic effect can occur [29,41,45]. A topical effect is desirable to skin diseases treatment [11,31,36,37] while a systemic effect is desirable to treat a more serious disease whose source is in another organ (i.e.…”

Section: Nanocarriers Bearing Citrus Oils or Citrus Terpenesmentioning

confidence: 99%

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Citrus Essential Oils and Nanosystems towards Skin Delivery

Santos¹,

Gonzatto²

2023

Citrus Research - Horticultural and Human Health Aspects

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Essentials oils from citrus have anti-inflammatory and antioxidant activity. Furthermore, terpenes are their main phytochemicals, namely limonene is the most important one. As terpenes are permeation promoters, they have been used to improve transdermal delivery of drugs. In addition, a proper oil source is a key factor to obtain desired phytochemicals. Recently, polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, liposomes and elastic liposomes as carriers of citrus essential oils or citrus terpenes have been developed to achieve more effective formulations. In this chapter, the most recent publications on nanocarriers containing citrus oils or citrus terpenes were addressed. In that regard, citrus oil or terpenes loaded in nanotechnological systems improve drugs skin permeation. Besides, terpenes loaded in nanoparticles also increase transdermal delivery of drugs. As essential oils and their respective terpenes are volatile compound and prone to oxidation, its encapsulations reduce oxidation and volatility. Hence, an improved antioxidant activity can be obtained. Therefore, nanoformulations of citrus oils or citrus terpenes are potential approaches to skin topical and transdermal delivery.

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Design of long acting invasomal nanovesicles for improved transdermal permeation and bioavailability of asenapine maleate for the chronic treatment of schizophrenia

Cited by 22 publications

References 30 publications

Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia

Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia

Chitosan Based Polyelectrolyte Complex Nanoparticles: Preparation and Characterization

Citrus Essential Oils and Nanosystems towards Skin Delivery

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