Transdermal delivery of second-generation antipsychotics for management of schizophrenia; disease overview, conventional and nanobased drug delivery systems

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

doi:10.1016/j.jddst.2020.102104

Cited by 9 publications

(3 citation statements)

References 73 publications

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“…As a result, it may restrict the amount of drugs that can be absorbed into the bloodstream when administered through the skin [15]. El-Tokhy et al concluded that the transdermal delivery of antipsychotics demonstrated improved therapeutic outcomes compared to oral administration [16]. However, formulations based on nanotechnology have provided several benefits and greater effectiveness compared to traditional methods.…”

Section: Introductionmentioning

confidence: 99%

The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride

Abdallah,

Shahien,

Alshammari

et al. 2024

Gels

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The present study explored the effectiveness of bile-salt-based nano-vesicular carriers (bilosomes) for delivering anti-psychotic medication, Sulpiride (Su), via the skin. A response surface methodology (RSM), using a 33 Box–Behnken design (BBD) in particular, was employed to develop and optimize drug-loaded bilosomal vesicles. The optimized bilosomes were assessed based on their vesicle size, entrapment efficiency (% EE), and the amount of Sulpiride released. The Sulpiride-loaded bilosomal gel was generated by incorporating the optimized Su-BLs into a hydroxypropyl methylcellulose polymer. The obtained gel was examined for its physical properties, ex vivo permeability, and in vivo pharmacokinetic performance. The optimum Su-BLs exhibited a vesicle size of 211.26 ± 10.84 nm, an encapsulation efficiency of 80.08 ± 1.88% and a drug loading capacity of 26.69 ± 0.63%. Furthermore, the use of bilosomal vesicles effectively prolonged the release of Su over a period of twelve hours. In addition, the bilosomal gel loaded with Su exhibited a three-fold increase in the rate at which Su transferred through the skin, in comparison to oral-free Sulpiride. The relative bioavailability of Su-BL gel was almost four times as high as that of the plain Su suspension and approximately two times as high as that of the Su gel. Overall, bilosomes could potentially serve as an effective technique for delivering drugs through the skin, specifically enhancing the anti-psychotic effects of Sulpiride by increasing its ability to penetrate the skin and its systemic bioavailability, with few adverse effects.

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Section: Introductionmentioning

confidence: 99%

The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride

Abdallah,

Shahien,

Alshammari

et al. 2024

Gels

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“…It could offer sustained release kinetics—especially for drugs with a short half-life—which, in turn, could reduce their dosing frequency. TDD is a drug delivery option that is characterized by patient acceptance and ease of application, leading to enhanced patient compliance, especially with chronic conditions such as schizophrenia [ 14 ].…”

Section: Introductionmentioning

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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“…In order to give full play to the advantages of transdermal drug delivery system (TDDS), continuous research is needed, to explore a variety of strategies to promote skin permeability. TDDS are being developed and studied in the treatment of obesity, Parkinsonism, diabetes, smoking cessation, analgesia, Alzheimer’s disease, hypertension, arthritis, osteoporosis, migraine, schizophrenia, and so on [ 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 ]. It is an excellent treatment especially for chronic diseases such as obesity that require long-term family treatment.…”

Section: Introductionmentioning

confidence: 99%

Transdermal Drug Delivery Systems and Their Use in Obesity Treatment

Fang

2021

IJMS

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Transdermal drug delivery (TDD) has recently emerged as an effective alternative to oral and injection administration because of its less invasiveness, low rejection rate, and excellent ease of administration. TDD has made an important contribution to medical practice such as diabetes, hemorrhoids, arthritis, migraine, and schizophrenia treatment, but has yet to fully achieve its potential in the treatment of obesity. Obesity has reached epidemic proportions globally and posed a significant threat to human health. Various approaches, including oral and injection administration have widely been used in clinical setting for obesity treatment. However, these traditional options remain ineffective and inconvenient, and carry risks of adverse effects. Therefore, alternative and advanced drug delivery strategies with higher efficacy and less toxicity such as TDD are urgently required for obesity treatment. This review summarizes current TDD technology, and the main anti-obesity drug delivery system. This review also provides insights into various anti-obesity drugs under study with a focus on the recent developments of TDD system for enhanced anti-obesity drug delivery. Although most of presented studies stay in animal stage, the application of TDD in anti-obesity drugs would have a significant impact on bringing safe and effective therapies to obese patients in the future.

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Transdermal delivery of second-generation antipsychotics for management of schizophrenia; disease overview, conventional and nanobased drug delivery systems

Cited by 9 publications

References 73 publications

The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride

The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride

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

Transdermal Drug Delivery Systems and Their Use in Obesity Treatment

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