Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone

Gu, Fei; Ma, Weina; Gao, Meng; Chunzhi, WU; Wang, Yi

doi:10.1515/acph-2016-0047

Cited by 8 publications

(3 citation statements)

References 13 publications

(10 reference statements)

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“…Disperse in each formula 45.5% W/V of the selected optimized Levetiracetam surfactant-based nano-vesicles. This was followed by adjusting the pH to approximately 6.0 using triethanolamine [21,22].…”

Section: Preparation Of Levetiracetam Surfactant-based Nanovesicles (...mentioning

confidence: 99%

Optimizing Levetiracetam Surfactant-Based Nanovesicles (Lev-Nvs) Gel for Treating Epilepsy Using Experimental Design

Teaima

MESSIRY²,

SHAKER³

et al. 2023

Int J App Pharm

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Objective: To develop and estimate the intranasal delivery of Levetiracetam surfactant-based nanovesicles (Lev-Nvs) as a brain-targeted antiepileptic delivery system prepared via solvent evaporation technique. Methods: Optimized formulation F (OPT) chosen by the Design-Expert® program gave the highest entrapment efficiency (EE%) was incorporated into the gel. An experimental design was adopted utilizing various (span 65) surfactants and different cholesterol ratios. The (Lev-Nvs) nanovesicles were formulated by solvent evaporation technique and evaluated for in vitro characterization parameters such as zeta sizer, Transmission Electron Microscopy (TEM), zeta potential. The nasal gel was evaluated for drug-excipient interactions utilizing Fourier Transform Infrared Spectroscopy (FTIR) and subjected to in vitro and in vivo release studies. Results: The results indicated that the entrapment efficiency (EE%) of Levetiracetam surfactant-based nano-vesicles (Lev-Nvs) could be modulated by the alterations in surfactant and cholesterol concentrations. Optimized formulation F (OPT) showed an entrapment efficiency of (87.9±1.06 %), (206.7±20.43 nm) particle size, (-34.1) zeta potential and (0.979) PDI. The nanovesicle nasal gels of the F(OPT) were prepared using Carbopol 940 at different concentrations. G 0.375 formulation showed the best in vitro drug release (87.36%) after 12 h. Finally, the comparative in vivo pharmaco-kinetics release studies on rats revealed considerable, sustained release of the nanovesicle nasal gel and higher relative bioavailability than an equivalent dose of oral solution (293.85%). Conclusion: Our study proves the improved efficacy of Levetiracetam as a surfactant-based nanovesicle intranasal gel in the brain targeting antiepileptic medication.

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Section: Preparation Of Levetiracetam Surfactant-based Nanovesicles (...mentioning

confidence: 99%

Optimizing Levetiracetam Surfactant-Based Nanovesicles (Lev-Nvs) Gel for Treating Epilepsy Using Experimental Design

Teaima

MESSIRY²,

SHAKER³

et al. 2023

Int J App Pharm

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“…Even if the addition of some excipients can easily be justified, scientists should be able to prove their safety, (Ingels et al, 1991;Schipper et al, 1991). Most frequently, the mucosa used for tolerance evaluations are not nasal mucosa but rather toad palate mucosa41, (Xie et al, 2006;Zhang et al, 2005;Gu et al, 2016). The test is usually performed on excised tissue but an alternative method is to deliver the formulation in vivo and recover the tissues after the animal sacrifice (Ument Karasulu et al, 2008).…”

Section: Determination Of the Formulation Tolerancementioning

confidence: 99%

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

Salade

Wauthoz

Goole

et al. 2019

International Journal of Pharmaceutics

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Nasal delivery offers many benefits over other conventional routes of delivery (e.g. oral or intravenous administration). Benefits include, among others, a fast onset of action, non-invasiveness and direct access to the central nervous system. The nasal cavity is not only limited to local application (e.g. rhinosinusitis) but can also provide direct access to other sites in the body (e.g. the central nervous system or systemic circulation). However, both the anatomy and the physiology of the nose impose their own limitations, such as a small volume for delivery or rapid mucociliary clearance. To meet nasal-specific criteria, the formulator has to complete a plethora of tests, in vitro and ex vivo, to assess the efficacy and tolerance of a new drug-delivery system. Moreover, depending on the desired therapeutic effect, the delivery of the drug should target a specific pathway that could potentially be achieved through a modified release of this drug. Therefore, this review focuses on specific techniques that should be performed when a nasal formulation is developed. The review covers both the tests recommended by regulatory agencies (e.g. the Food and Drug Administration) and other complementary experiments frequently performed in the field.

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“…However, the chemical stability and microbial stability of powder spray are higher than those of liquid spray. Moreover, because of longer retention time in vivo and Advances in Social Science, Education and Humanities Research,volume 78 contact time with nasal mucosa, the bioavailabilities of powder formulations and gel formulations were higher than those of liquid formulations (F. Gu et al 6 , L. Illum 7 and S.…”

mentioning

confidence: 99%

Therapeutic Effect of a Novel Human Parathyroid Hormone Analog Nasal Drops on Osteoporosis Rats

Jiao¹,

Zhu²,

Gao³

et al. 2017

Proceedings of the International Conference on Social Science, Public Health and Education (SSPHE 2017)

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In this study, the therapeutic effect of a novel human parathyroid hormone analogs nasal drops on ovariectomized rats was evaluated. Thirty-two of 40 3-month-old female Sprague-Dawley rats were ovariectomized and 8 received sham operation. Thirteen weeks later, ovariectomized rats were randomly and averagely divided into 4 groups: low dose, middle dose and high dose group (31.25, 125, 500 μg/rat respectively) and vehiculum group (0.5 mL/rat). Each group was administered to the nasal drops. Another 8 sham-operated rats were treated in the same way as those of vehiculum group. All rats were administered daily. After 16 weeks of continuous administration, the osteogenic ability was compared between rats in each group. The results indicated that compared with vehiculum group, significant increments in the dry weights of femur, trabecular area and trabecular width were shown in the groups treated with middle dose and high dose hPTH'. The results showed dose dependence. It is concluded that hPTH' nasal drop is effective in stimulating bone formation and improving skeletal microarchitecture and potentially an effective therapeutical agent on osteoporosis.

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Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone

Cited by 8 publications

References 13 publications

Optimizing Levetiracetam Surfactant-Based Nanovesicles (Lev-Nvs) Gel for Treating Epilepsy Using Experimental Design

Optimizing Levetiracetam Surfactant-Based Nanovesicles (Lev-Nvs) Gel for Treating Epilepsy Using Experimental Design

How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods

Therapeutic Effect of a Novel Human Parathyroid Hormone Analog Nasal Drops on Osteoporosis Rats

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