scholarly journals In Vitro Drug Release and Ex Vivo Permeation Study of Prepared Mouth Dissolving Tablets of Fluconazole Through Porcine Buccal Mucosa

2014 ◽  
Vol 17 (7) ◽  
pp. A739-A740
Author(s):  
T Chakraborty ◽  
V Saini
Keyword(s):  
Drug Release ◽  
Buccal Mucosa ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study

scholarly journals FORMULATION OF KETOCONAZOLE LOADED NANO DISPERSIVE GEL USING SWOLLEN MICELLES TECHNIQUE AND ITS IN VITRO CHARACTERIZATION

2018 ◽  
Vol 10 (3) ◽  
pp. 162
Author(s):  
Mohammad Irshad Reza ◽  
Divya Goel ◽  
Rahul Kumar Gupta ◽  
Musarrat Hussain Warsi
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Enhanced Solubility ◽  
Ex Vivo Permeation Study

Objective: The objective of the present work was to formulate and characterize nano dispersive gel (NDG) for topical delivery of water-insoluble antifungal agent ketoconazole in order to enhance its solubility, penetration through the skin and antifungal activity.Methods: Nano dispersion of the drug was first prepared by swollen micelles technique (SMT) using tween 80 and chloroform which is then incorporated into the gel using carbopol 934. Ten formulations of ketoconazole loaded NDG was prepared and characterized for different physicochemical parameters like homogeneity, pH, spreadability, extrudability, practical yield, drug content, in vitro drug release, ex vivo permeation study, and biological parameter antifungal activity.Results: The formulated topical preparation exhibit pH in the range of 6.5 to 7.4, and unveiled excellent homogeneity, spreadability and extrudability. Out of 10 formulations, formulation F4 showed maximum drug content of 95.56±1.13% and practical yield of 97.23±0.51%. The in vitro drug release studies were performed using pH 7.4 phosphate buffer. Formulation F4 showed best in vitro drug release 96.52±0.52% at the end of 24 h of study. Ex vivo permeation study of formulation F4 carried out using franz diffusion cell, also manifested good permeation and flux of drug across the chicken skin. Antifungal activity test of formulation F4 was carried out by the cup plate method using Aspergillus niger strain against marketed ketoconazole unveiled higher antifungal activity than marketed one.Conclusion: The study confirmed formulation F4 to be an optimized and promising formulation for the effective treatment of topical fungal infections with enhanced solubility and penetration through the skin.

scholarly journals Formulation and Evaluation of Tacrolimus Transdermal Gel

2019 ◽  
Vol 9 (6-s) ◽  
pp. 110-118
Author(s):  
CH. Suryakumari ◽  
M. Narender ◽  
K. Umasankar ◽  
Siva Prasad Panda ◽  
S.N. Koteswara Rao ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Abdominal Skin ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study ◽  
Carbopol 934P

The present investigation is concerned with formulation and evaluation of Transdermal gels of Tacrolimus, anti-psoriasis drug, to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. Twelve formulations were developed with varying concentrations of polymers like Carbopol 934P, HPMCK4M and Sodium CMC. The gels were tested for clarity, Homogeneity, Spreadability, Extrudability, Viscosity, surface pH, drug Content uniformity, in-vitro drug diffusion study and ex-vivo permeation study using rat abdominal skin. FTIR studies showed no evidence on interactions between drug, polymers and excipients. The best in-vitro drug release profile was achieved with the formulation F4 containing 0.5 mg of exhibited 6 hr drug release i.e. 98.68 % with desired therapeutic concentration which contains the drug and Carbopol 934p in the ratio of 1:2. The surface pH, drug content and viscosity of the formulation F4 was found to be 6.27, 101.3% and 3, 10,000cps respectively. The drug permeation from formulation F4 was slow and steady and 0.89gm of tacrolimus could permeate through the rat abdominal skin membrane with a flux of 0.071 gm hr-1 cm-2. The in-vitro release kinetics studies reveal that all formulations fit well with zero order kinetics followed by non-Fickian diffusion mechanism. Keywords: Transdermal gel, Viscosity, In-vitro drug release, In-vitro drug release kinetics study, Ex-vivo permeation study

scholarly journals Formulation and Evaluation of Sustained Release Sumatriptan Mucoadhesive Intranasal in-Situ Gel

2019 ◽  
Vol 28 (2) ◽  
pp. 95-104
Author(s):  
Hussein K. Alkufi ◽  
Hanan J. Kassab
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Ex Vivo Permeation ◽  
Ex Vivo Permeation Study

     Objective: The purpose of this study to develop and optimize nasal mucoadhesive in situ gel IG of sumatriptan ST (serotonin agonist) to enhance nasal residence time for migraine management.      Method: Cold method was used to prepare ST nasal in-situ gel, using thermosensitive polymers (poloxamer 407  and/or poloxamer 188) with a mucoadhesive polymer (hyaluronic acid HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, mucoadhesive force determination, viscosity,  in-vitro drug release, and the selected formula was subjected to ex-vivo permeation study and histological evaluation of the sheep mucosal tissue after application.     Results: The results showed that the formula IG7 prepared from poloxamer 407(19%), poloxamer188 (4%) and HA (0.5%)   had an optimum gelation temperature (32.66±1.52°C), gel  strength (43.66± 1.52 sec),  mucoadhesive force (8067.93± 746.45dyne\cm2), in-vitro drug release (95.98%) over 6hr, ex-vivo permeation study release (89.6%)  during the 6 h. study with no  histological or pathological change in the nasal sheep tissue.     Conclusion: The ease of administration via a nasal drop of ST coupled with less frequent administration and prolong drug release, will enhance patient compliance.

Transdermal Delivery of Ondansetron HCl from Thermoreversible Gel Containing Nanocomposite

2019 ◽  
Vol 4 (2) ◽  
pp. 137-147 ◽  
Author(s):  
Rabinarayan Parhi ◽  
Surya Santhosh Reddy ◽  
Suryakanta Swain
Keyword(s):  
Drug Release ◽  
Mechanical Strength ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Model Animal ◽  
Ex Vivo Permeation Study ◽  
Thermoreversible Gel

Background: Application of thermoreversible gel can be a solution to the low residence time of the topical dosage forms such as normal gel, ointment and cream on the skin surface. Addition of another polymer and a nanocomposite can improve the poor mechanical strength and fast drug release of poloxamer 407 (POL 407) gel. Therefore, it is essential to add xanthan gum (XG) and graphene oxide (GO, thickness 1-2 nm, lateral dimension 1-5 µm) to POL 407 gel to enhance the mechanical strength and to sustain the drug release from the gel. Methods: Thermal gel of ondansetron hydrochloride (OSH) containing nanocomposite was prepared by adopting cold method. Interaction between drug and polymers was studied using FTIR method, morphological investigation was carried out by optical and scanning electron microscopy method, and rheological study was performed employing rotational rheometer equipped with a cone/plate shear apparatus, gelation temperature by glass bottle method and ex vivo permeation study was performed with cylindrical glass diffusion cell. Skin irritation potential was measured using rat as a model animal. Results: The FTIR spectrum of the selected gel showed that there is shifting of O-H stretching vibration of a hydroxyl group from 3408.72 to 3360.49 cm-1 and appearance of a new band at 1083.01 cm-1. The spectrum of the selected gel also showed the absence of characteristic peaks of GO at 1625.49 cm- 1. This result indicated that there may be an interaction between OSH and GO and hydrogen bonding between XG and POL 407. The gelation temperature was found to be decreased with the increase in GO content from 14.1±1.21°C 13±0.97°C. SEM micrograph demonstrated the uniform dispersion and intercalation of GO sheets in the gel. All the gel formulations showed a pseudo-plastic flow. Ex vivo permeation study (for 24 hr) exhibited highest (6991.425 µg) and lowest (2133.262 µg) amount of drug release, for OG1 and OG5, respectively. This is attributed to an increase in viscosity which led to a decrease in drug permeation across the abdominal skin of rats. The OG1 formulation (without GO) showed the highest flux of 76.66 µg/cm2/h, permeability coefficient (Kp) of 5.111× 10-3 cm/h and enhancement ratio of 3.277 compared to OG5 containing highest amount (9% w/w) of GO. The selected gel was found to be physically stable and there was minimum irritation score. Conclusion: All the above results indicated that thermal gel containing nanocomposite sustained the drug release and can be considered as an alternative to the orally administered tablet of OSH.

scholarly journals Exploration of neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex based film for transdermal delivery of protein/peptide

2020 ◽  
Vol 10 (4) ◽  
pp. 5860-5868
Keyword(s):  
Drug Release ◽  
Drug Concentration ◽  
Polyelectrolyte Complex ◽  
Ex Vivo ◽  
Extended Period ◽  
In Vitro Drug Release ◽  
Drug Permeation ◽  
Permeation Study ◽  
Weight Variation

Present investigation is continuation of author’s previously published work. In the present investigation, the author has prepared neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex transdermal film for the delivery of protein/peptide drug. Concentration of gum (neem gum and kheri gum) and chitosan was varied in each concentration while drug concentration kept constant. Albumin was used as a model protein drug. Transdermal films were fabricated using a solvent casting method without using any plasticizer and evaluated for various parameters viz. folding endurance, surface pH, weight variation, drug content, percentage moisture content, surface morphology, in vitro drug release and ex vivo drug permeation study. The study showed that films were successfully fabricated with good acceptable physical properties. In vitro drug release study and ex vivo drug permeation study showed that polyelectrolyte films were able to extend drug delivery up to 9 days. It can be easily concluded from the findings of the results that neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex films can be easily prepared without using any plasticizer and able to deliver protein/peptide therapeutic agents for an extended period of time.

scholarly journals Formulation and Evaluation of Clarithromycin Loaded Nanostructured Lipid Carriers for the Treatment of Acne

2021 ◽  
pp. 26-38
Author(s):  
Pooja Shettigar ◽  
Marina Koland ◽  
S. M. Sindhoor ◽  
Ananth Prabhu
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Acne Treatment

Background: Clarithromycin is a macrolide antibiotic used in acne treatment, but it has poor solubility, which decreases its permeability through lipid barriers such as skin. Nanostructured lipid carriers can enhance the permeability of clarithromycin through the skin, thus improving its potential for controlling acne. Aim: To formulate and evaluate Nanostructured lipid carriers of clarithromycin for topical delivery in acne treatment Methods: Nanostructured lipid carriers were prepared by emulsification and ultrasonication methods using lipids such as glycerol monostearate and oleic with poloxamer 188 as stabilizer. These nano-carriers were optimized with the help of the Quality by Design (QbD) approach employing Design-Expert® software. The nanoparticles were characterized for particle size analysis, zeta potential, drug-excipient compatibility, entrapment efficiency, and surface morphology by Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The nano-carriers were also investigated for in vitro drug release and ex vivo permeation through excised goat skin. The optimized formulation was incorporated into topical carbopol gel base, formulated and examined for pH, viscosity, spreadability, in vitro drug release, ex vivo permeation, and stability under accelerated conditions. Results: The average particle size of the optimized nanoparticles was 164.8 nm, and zeta potential was -39.2 mV. FTIR studies showed that drug and lipids are compatible with each other. The morphology study by SEM and TEM showed spherical shaped particles. The entrapment efficiency of the optimized formulation was found to be 88.16%. In vitro drug release studies indicated sustained release from the formulation due to diffusion through the lipid matrix of the particles. The ex vivo permeation study using goat skin produced greater permeation from the NLC gel (89.5%) than marketed gel (65%) due to the lipid solubility of the nanoparticles in the skin. The formulation was stable under accelerated conditions. Conclusion: The optimized formulation can be considered as promising nano-carriers suitable for the sustained release of clarithromycin into the skin for effective control of acne.

scholarly journals FORMULATION AND EVALUATION OF LORAZEPAM ENCAPSULATED COLLAGEN/PECTIN BUCCAL PATCH

2019 ◽  
pp. 200-209
Author(s):  
LAKSHMI V. S. ◽  
REVATHY B. MENON ◽  
KEERTHANA RAJU ◽  
AISWARYA M. U. ◽  
SREEJA C. NAIR
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Epileptic Seizures ◽  
Stability Study ◽  
Histopathological Study ◽  
In Vitro Drug Release ◽  
Control Drug ◽  
Ex Vivo Permeation Study ◽  
The Stability

Objective: To formulate and characterize Lorazepam loaded buccal patches using mucoadhesive, biodegradable, natural polymers-pectin (hydrophilic) and collagen (lipophilic) for treating epileptic seizures. Methods: Lorazepam loaded buccal patches were prepared by solvent casting method and were subjected to various Physico-chemical evaluation parameters to find the optimized buccal patch. The in vitro drug release study and ex vivo permeation study was carried out. The stability study and histopathological study of optimized Lorazepam loaded buccal patch was also carried out. Results: From in vitro drug release study, it was found that Lorazepam loaded buccal patch (B4) exhibited maximum drug release of 96.16 %±0.07 than other formulations at the end of 4 h, indicating an initial burst release followed by sustained release with release kinetics as Higuchi diffusion model. Based on the in vitro drug release, % drug content, % swelling index, folding endurance, B4 formulation was considered as optimised formulation and was further characterized. Ex vivo permeation study revealed that the cumulative amount of drug permeated from optimised Lorazepam loaded buccal patch (B4) was higher (3831.4±0.21µg/cm2) than marketed Midazolam buccal solution (1724±0.12 µg/cm2) and control drug solution (895.42±0.07 µg/cm2) with an enhancement ratio of 4.8. B4 formulation also showed a higher flux value (12.52±0.02µg/cm2/hr) compared to marketed formulation (5.732±0.01 µg/cm2) and control drug solution (2.563±0.03 µg/cm2) of P<0.05. The histopathological study using bovine buccal mucosa revealed that the B4 formulation is safe for buccal application. The stability study confirmed that B4 formulation is stable in both room and refrigeration conditions. Hence the formulated Lorazepam loaded buccal patch seems to be a promising carrier for the enhanced buccal delivery of Lorazepam in treating epileptic seizures. Conclusion: The formulated Lorazepam loaded collagen/pectin buccal patch was found to be an efficient and stable route for the buccal delivery of Lorazepam in treating acute epileptic seizures which could be further explored scientifically.

scholarly journals MUCOADHESIVE POLYMERIC FILMS OF ACYCLOVIR PRONIOSOMES FOR BUCCAL ADMINISTRATION

2021 ◽  
pp. 135-143
Author(s):  
DEEKSHA U. SUVARNA ◽  
MARINA KOLAND ◽  
ANANTH PRABHU ◽  
SINDHOOR S. M.
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Polymeric Films ◽  
Prolonged Release ◽  
Mucosal Permeability ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Span 60

Objective: The aim of the present work was to formulate and evaluate proniosomes of the poorly soluble drug, acyclovir incorporated in mucoadhesive polymeric films for improved buccal mucosal permeability of the drug while achieving prolonged release. Methods: Acyclovir was formulated as proniosomes using Span 60 and cholesterol. The prepared proniosomes were loaded into mucoadhesive polymeric films prepared with varying quantities of carbopol 934P and HPMC K15M. The proniosome incorporated films were evaluated for physicomechanical characters, mucoadhesion, swelling index, drug content, in vitro drug release and ex vivo permeation through porcine buccal mucosa. Results: Hydration of the proniosomes produced spherical vesicles or niosomes, which was confirmed by Scanning Electron Microscopy. The optimized formulation selected on the basis of vesicle size, entrapment efficiency PDI, Zetz potential and in vitro drug release was selected for incorporation into mucoadhesive polymeric films. All the films showed excellent physicomechanical characters. Formulations with higher proportions of carbopol produced slower in vitro drug release. The kinetics of release of drug from all the formulations appeared to be zero-order based on their regression coefficient values. Comparative evaluation of ex vivo permeation from niosomal and non-niosomal films indicated that the former demonstrated improved mucosal permeation and drug release was also sustained for the 8 h period. Conclusion: Mucoadhesive films impregnated with acyclovir loaded proniosomes could be a potential approach for buccal delivery of acyclovir for improving its absorption and bioavailability. 

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.

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