Development of a liquid chromatographic method for the quantification of paromomycin. Application to in vitro release and ex vivo permeation studies

2014 ◽  
Vol 133 ◽  
pp. 657-662 ◽  
Author(s):  
A. Pujol-Brugués ◽  
A.C. Calpena-Campmany ◽  
C. Riera-Lizandra ◽  
L. Halbaut-Bellowa ◽  
B. Clares-Naveros
Keyword(s):  
Chromatographic Method ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Ex Vivo Permeation ◽  
Liquid Chromatographic Method ◽  
Permeation Studies ◽  
Liquid Chromatographic ◽  
Vitro Release

Nanostructured Lipid Carriers for Intranasal Administration of Olanzapine in the management of Schizophrenia

2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Poloxamer 407 ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Vitro Release

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.

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.

scholarly journals NOVEL NANOPARTICLES FOR THE ORAL DELIVERY OF LOW MOLECULAR WEIGHT HEPARIN: IN VITRO AND IN VIVO ASSESSMENT

2017 ◽  
Vol 10 (2) ◽  
pp. 254 ◽  
Author(s):  
Nallaguntla Lavanya ◽  
Indira Muzib ◽  
Aukunuru Jithan ◽  
Balekari Umamahesh
Keyword(s):  
Molecular Weight ◽  
Low Molecular Weight Heparin ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Low Molecular Weight ◽  
Scanning Calorimetry ◽  
Ex Vivo Permeation ◽  
Permeation Studies

Objective: The objective of the present study was to prepare and evaluate a novel oral formulation of nanoparticles for the systemic delivery of low molecular weight heparin (LMWH). Methods: Nanoparticles were prepared by polyelectrolyte complexation (PEC) method using polymers sodium alginate and chitosan. Entrapment efficiency of LMWH in nanoparticles was found to be  ̴88%. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X‑ray diffraction (XRD), Scanning electron microscopy (SEM)  studies carried for nanoparticles. In vitro release studies were performed for the formulations. Ex vivo permeation studies were performed optimized formulation by using small intestine of rat and in vivo studies were conducted on rat model.Results: In vitro release studies demonstrated that the release of LMWH was negligible in the stomach and high in the small intestine. FTIR has indicated that there is no interaction between the ingredients in nanoparticle. DSC and XRD studies confirmed that the amino groups of chitosan interacted with the carboxylic groups of alginate. Invitro % drug release of 95% was shown by formulation AC5. Ex vivo permeation studies have elucidated that ̴ 73% of LMWH was transported across the epithelium. Nanoparticles have shown enhanced oral bioavailability of LMWH as revealed by 4.5 fold increase in AUC of plasma drug concentration time curve.Conclusion: The results suggest that the nanoparticles prepared can result in targeted delivery of LMWH into systemic circulation via intestinal and colon routes. Novel nanoparticles thus prepared in this study can be considered as a promising delivery system.Keywords: Antifactor Xa activity, Chitosan, Differential scanning calorimetry, Sodium alginate, Low-molecular-weight heparin, Oral bioavailability.

scholarly journals Development of Itraconazole-Loaded Polymeric Nanoparticle Dermal Gel for Enhanced Antifungal Efficacy

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Hoang Nhan Ho ◽  
Thien Giap Le ◽  
Thi Thanh Tuyen Dao ◽  
Thi Ha Le ◽  
Thi Thanh Hai Dinh ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Polymeric Nanoparticle ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Gel Formulations ◽  
In Vitro Antifungal Activity ◽  
Better Than

Fungal infection of the skin is one of the most common dermatological diseases in the world. Gel formulations are among the most suitable dosage forms for topical use to treat cutaneous infection. Nanotechnology is a promising approach to penetrate the deeper skin layers and enhance permeability of itraconazole (ITZ) through the stratum corneum. ITZ-loaded nanoparticles (ITZ NPs) were fabricated using the evaporation emulsion method, followed by incorporation of NPs into gel using Carbopol 934 as the gel-forming excipient. The physical properties, in vitro release, ex vivo permeation studies, and antifungal activity of ITZ NP gel were characterized. ITZ NPs were almost spherical in shape with colloidal sizes in the range of 200 nm. The drug encapsulation efficiency was 98.79 ± 1.24 %. ITZ NP gel demonstrated a sustained ex vivo permeation of ITZ over 24 h through excised rat skin and a higher drug penetrating capacity than that of a gel containing ITZ-saturated suspension. The in vitro antifungal activity of the ITZ-loaded NP incorporated gel was better than that of ITZ dispersion. Incorporation of the ITZ-loaded nanosystem into gel has the potential to enhance antifungal activity through transdermal drug delivery.

Improved in vitro Release and ex vivo Permeation of Zotepine as Microemulsion Gel Formulation through Transdermal Application

2021 ◽  
Vol 14 (1) ◽  
pp. 5343-5352
Author(s):  
Akhila Keshoju ◽  
Dinesh Suram ◽  
Chandra Mouli Golla ◽  
Nagaraj B
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Gelling Agent ◽  
Prolonged Release ◽  
Rat Skin ◽  
Skin Delivery ◽  
Ex Vivo Permeation ◽  
Vitro Release ◽  
Microemulsion Gel

Zotepine is atypical antipsychotic drug with poor oral bioavailability due to first-pass metabolism and poor aqueous solubility. The objective of the current investigation was preparation and ex vivo characterization of Zotepine (ZT) loaded microemulsion (ZT-ME) and microemulsion gel (ZT-MEG) for enhanced transdermal delivery.  ZT-ME formulation was prepared with 7.5% oleic acid, 30% w/v of Tween80 and 30%w/v of absolute ethanol as oil, surfactant and cosurfactant, respectively. Optimized ZT-ME formulation was selected and converted to ZT-MEG using carbopol as gelling agent. ZT-ME and ZT-MEG subjected to in vitro release and ex vivo permeation studies through rat skin, comparison with ZT coarse suspension (ZT-CS). ZT-ME formulation showed desirable physicochemical properties and stable with dilution stress. Prepared ZT-MEG formulation has showed better rheological behaviour and good spreadability. ZT-ME and ZT-MEG showed prolonged release compared with ZT-CS formulation over 24 h. ZT-ME and ZT-MEG exhibited 5-folds and 3.5-folds in permeation through rat skin compared with ZT-CS formulation. Overall, ZT-MEG formulation could be considered as an alternative delivery approach for enhanced skin delivery. 

STUDIES ON NANOLIPID EMULGEL OF NIMESULIDE FOR TRANSDERMAL DELIVERY

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (09) ◽  
pp. 74-77
Author(s):  
C Trimukhe ◽  
P. Patil ◽  
K. Sheth ◽  
N. Desai ◽  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Spherical Particles ◽  
Sustained Drug Release ◽  
Polyethylene Glycol 400 ◽  
Ex Vivo Permeation ◽  
Nanometric Range ◽  
Permeation Studies

The objective of the present study was to develop and evaluate a nanolipid transdermal emulgel of Nimesulide. The nanolipid particles of Nimesulide were developed using Compritol 888 ATO and Labrafil M1944 as lipids, Polysorbate 80 as surfactant with Poloxamer 188 and Polyethylene Glycol 400 as stabilizer and cosolvent respectively. The nanoparticles were developed by Hot Nanoemulsification Low Temperature Solidification method and showed drug entrapment efficiency of 67 ± 2.316 % with particle size of 500 – 600 nm. TEM studies indicated presence of spherical particles in the nanometric range. The nanolipidic dispersions were suitably gelled to form emulgel. The in vitro release of the developed emulgel showed sustained drug release for 8 hours with no evidence of toxicity during histopathological testing after ex vivo permeation studies. The nanolipid emulgel of Nimesulide can thus provide sustained release action due to enhanced skin deposition for effective treatment of chronic arthritic conditions, thereby improving patient compliance.

scholarly journals Development of Tizanidine HCl transdermal patches: In-vitro and Ex-vivo characterization

2019 ◽  
Vol 9 (1-s) ◽  
pp. 295-300
Author(s):  
Dr. Shayeda ◽  
Nusrat Ayesha
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Transdermal Patches ◽  
Ex Vivo Permeation ◽  
Release Studies ◽  
Transdermal Drug Delivery Systems ◽  
Folding Endurance ◽  
Vitro Release

The purpose of this work was to design and evaluate matrix type transdermal patches of Tizanidine hydrochloride using Hypromellose (HPMC E15) as polymer, dibutyl phthalate as plasticizer and citral as permeation enhancer. The DSC and FTIR results showed the compatibility of the excipients with the drug. These transdermal drug delivery systems were characterized for their thickness, folding endurance, content uniformity, tensile strength and in-vitro release studies of the drug from the polymeric matrix. In-vitro release studies and ex-vivo permeation were carried out with modified Franz diffusion cell using pH 5.8 & pH 7.4 phosphate buffers as receptor medium and it showed controlled release of drug. The results suggest that the formulation of TIZ may be useful in the development of a therapeutic system to deliver TIZ across the skin for a prolonged period, i.e. 24 hr. Keywords: Tizanidine Hydrochloride, Transdermal patch, HPMC E15, in-vitro & ex-vivo.

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