Formulation and optimization of terbinafine HCl loaded chitosan/xanthan gum nanoparticles containing gel: Ex-vivo permeation and in-vivo antifungal studies

2021 ◽  
pp. 102935
Author(s):  
Fahad Pervaiz ◽  
Rabia Mushtaq ◽  
Sobia Noreen
Keyword(s):  
Xanthan Gum ◽  
Ex Vivo ◽  
Ex Vivo Permeation ◽  
Terbinafine Hcl

Development, Pre-clinical Investigation and Histopathological Evaluation of Metronidazole Loaded Topical Formulation for Treatment of Skin Inflammatory disorders

2020 ◽  
Vol 10 ◽  
Author(s):  
Divya Thakur ◽  
Gurpreet Kaur ◽  
Sheetu Wadhwa ◽  
Ashana Puri
Keyword(s):  
Ex Vivo ◽  
Clinical Investigation ◽  
In Vivo Studies ◽  
Tween 20 ◽  
Inflammatory Disorders ◽  
Rat Paw Edema ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Metronidazole (MTZ) is an anti-oxidant and anti-inflammatory agent with beneficial therapeutic properties. The hydrophilic nature of molecule limits its penetration across the skin. Existing commercial formulations have limitations of inadequate drug concentration present at target site, which requires frequent administration and poor patient compliance. Objective: The aim of current study was to develop and evaluate water in oil microemulsion of Metronidazole with higher skin retention for treatment of inflammatory skin disorders. Methods: Pseudo ternary phase diagrams were used in order to select the appropriate ratio of surfactant and co-surfactant and identify the microemulsion area. The selected formulation consisted of Capmul MCM as oil, Tween 20 and Span 20 as surfactant and co-surfactant, respectively, and water. The formulation was characterized and evaluated for stability, Ex vivo permeation studies and in vivo anti-inflammatory effect (carrageenan induced rat paw edema, air pouch model), anti-psoriatic activity (mouse-tail test). Results: The particle size analyses revealed average diameter and polydispersity index of selected formulation to be 16 nm and 0.373, respectively. The results of ex vivo permeation studies showed statistically higher mean cumulative amount of MTZ retained in rat skin from microemulsion i.e. 21.90 ± 1.92 μg/cm2 which was 6.65 times higher as compared to Marketed gel (Metrogyl gel®) with 3.29 ± 0.11 μg/cm2 (p<0.05). The results of in vivo studies suggested the microemulsion based formulation of MTZ to be similar in efficacy to Metrogyl gel®. Conclusion: Research suggests efficacy of the developed MTZ loaded microemulsion in treatment of chronic skin inflammatory disorders.

In vivo distribution and ex vivo permeation of cyclosporine A prodrug aqueous formulations for ocular application

2013 ◽  
Vol 170 (1) ◽  
pp. 153-159 ◽  
Author(s):  
Marta Rodriguez-Aller ◽  
Davy Guillarme ◽  
Mohamed El Sanharawi ◽  
Francine Behar-Cohen ◽  
Jean-Luc Veuthey ◽  
...  
Keyword(s):  
Cyclosporine A ◽  
Ex Vivo ◽  
In Vivo Distribution ◽  
Ex Vivo Permeation

scholarly journals Ex Vivo Permeation of Carprofen Vehiculated by PLGA Nanoparticles through Porcine Mucous Membranes and Ophthalmic Tissues

Nanomaterials ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 355 ◽  
Author(s):  
Lídia Gómez-Segura ◽  
Alexander Parra ◽  
Ana Cristina Calpena-Campmany ◽  
Álvaro Gimeno ◽  
Immaculada Gómez de Aranda ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Cell Structure ◽  
Topical Administration ◽  
Plga Nanoparticles ◽  
In Vivo Studies ◽  
Ex Vivo Permeation ◽  
Mucous Membranes ◽  
Anti Inflammatory ◽  
Almost All

(1) Background: Carprofen (CP), 2-(6-chlorocarbazole) propionic acid, is used as an anti-inflammatory, analgesic and anti-pyretic agent and it belongs to the family of non-steroidal anti-inflammatory drugs (NSAIDs). CP has some adverse reactions in systemic administration; for this reason, topical administration with CP nanoparticles (CP-NPs) can be an optimal alternative. The main objective of this work is the investigation of ex vivo permeation of CP through different types of porcine mucous membranes (buccal, sublingual and vaginal) and ophthalmic tissues (cornea, sclera and conjunctiva) to compare the influence of CP-NPs formulation over a CP solution (CP-Solution). (2) Methods: The ex vivo permeation profiles were evaluated using Franz diffusion cells. Furthermore, in vivo studies were performed to verify that the formulations did not affect the cell structure and to establish the amount retained (Qr) in the tissues. (3) Results: Permeation of CP-NPs is more effective in terms of drug retention in almost all tissues (with the exception of sclera and sublingual). In vivo studies show that neither of the two formulations affects tissue structure, so both formulations are safe. (4) Conclusions: It was concluded that CP-NPs may be a useful tool for the topical treatment of local inflammation in veterinary and human medicine.

scholarly journals Formulation Development of Sublingual Cyclobenzaprine Tablets Empowered by Standardized and Physiologically Relevant Ex Vivo Permeation Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1409
Author(s):  
Haidara Majid ◽  
Andreas Puzik ◽  
Tanja Maier ◽  
Raphaela Merk ◽  
Anke Bartel ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vivo Studies ◽  
Process Automation ◽  
Formulation Development ◽  
Tissue Integrity ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
The Impact

Suitable ex vivo models are required as predictive tools of oromucosal permeability between in vitro characterizations and in vivo studies in order to support the development of novel intraoral formulations. To counter a lack of clinical relevance and observed method heterogenicity, a standardized, controlled and physiologically relevant ex vivo permeation model was established. This model combined the Kerski diffusion cell, process automation, novel assays for tissue integrity and viability, and sensitive LC-MS/MS analysis. The study aimed to assess the effectiveness of the permeation model in the sublingual formulation development of cyclobenzaprine, a promising agent for the treatment of psychological disorders. A 4.68-fold enhancement was achieved through permeation model-led focused formulation development. Here, findings from the preformulation with regard to pH and microenvironment-modulating excipients proved supportive. Moreover, monitoring of drug metabolism during transmucosal permeation was incorporated into the model. In addition, it was feasible to assess the impact of dosage form alterations under stress conditions, with the detection of a 33.85% lower permeation due to salt disproportionation. Integrating the coherent processes of disintegration, dissolution, permeation, and metabolization within a physiological study design, the model enabled successful formulation development for cyclobenzaprine sublingual tablets and targeted development of patient-oriented drugs for the oral cavity.

Formulation and Evaluation of Neuroactive Drug Loaded Chitosan Nanoparticle for Nose to Brain Delivery: In-vitro Characterization and In-vivo Behavior Study

2018 ◽  
Vol 16 (2) ◽  
pp. 123-135 ◽  
Author(s):  
Mohsin Qureshi ◽  
Mohd. Aqil ◽  
Syed Sarim Imam ◽  
Abdul Ahad ◽  
Yasmin Sultana
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Drug Loading ◽  
Brain Delivery ◽  
Permeation Study ◽  
Behavior Study ◽  
Ex Vivo Permeation ◽  
Chitosan Nanoparticle ◽  
Ex Vivo Permeation Study

Background: The present work was designed to explore the efficacy of neuroactive drug (risperidone) loaded chitosan lipid nanoparticle (RIS-CH-LNPs) to enhance the bioactivity in schizophrenia via the nasal route. </P><P> Methods: The three-factor and three-level formulation by design approach was used for optimization and their effects were observed on (Y1) size in nm, (Y2) % drug loading, and (Y3) % drug release. The optimized formulation RIS-CH-LNPopt was further evaluated for its surface morphology, ex-vivo permeation study, in-vivo behavior study, and stability study. The developed RIS-CH-LNPs showed nanometric size range with high drug loading and prolonged drug release. Results: The optimized formulation (RIS-CH-LNPopt) has shown the particle size (132.7 nm), drug loading (7.6 %), drug release (80.7 %) and further ex-vivo permeation study showed 2.32 fold enhancement over RIS-SUS(suspension). In-vivo behavior studies showed that RIS-CH-LNPopt is able to show significant greater bioefficacy as compared to RIS-SUS [intranasal (i.n), intravenous (i.v)]. The pharmacokinetic and brain/plasma ratio of developed chitosan nanoparticle was higher at all time-points as compared to RIS-SUS either given by intranasal or intravenous route that proves the direct nose to brain transport pathway of the drug via nasal administration. The developed chitosan nanoparticle increases nose to brain drug delivery as compared to the dispersion of equivalent dose. The findings of this study substantiate the existence of a direct nose-to-brain delivery route for RIS-CH-LNPs.

scholarly journals Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 64 ◽  
Author(s):  
Lupe Carolina Espinoza ◽  
Marcelle Silva-Abreu ◽  
Beatriz Clares ◽  
María José Rodríguez-Lagunas ◽  
Lyda Halbaut ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Release Profile ◽  
In Vivo Models ◽  
Tablet Form ◽  
Ex Vivo Permeation ◽  
Vitro Release

Donepezil (DPZ) is widely used in the treatment of Alzheimer’s disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood–brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Composition of NE was established using three pseudo-ternary diagrams and PNE was developed by incorporating Pluronic F-127 to the aqueous phase. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined for both formulations. The tolerability was evaluated by in vitro and in vivo models. DPZ-NE and DPZ-PNE were transparent, monophasic, homogeneous, and physically stable with droplets of nanometric size and spherical shape. DPZ-NE showed Newtonian behavior whereas a shear thinning (pseudoplastic) behavior was observed for DPZ-PNE. The release profile of both formulations followed a hyperbolic kinetic. The permeation and prediction parameters were significantly higher for DPZ-PNE, suggesting the use of polymers to be an effective strategy to improve the bioadhesion and penetration of the drug through nasal mucosa, which consequently increase its bioavailability.

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