scholarly journals FORMULATION AND EVALUATION OF IVABRADINE HYDROCHLORIDE LOADED TRANSFERSOMAL GEL FOR TRANSDERMAL DELIVERY

2020 ◽  
pp. 295-301
Author(s):  
GITA CHAURASIA ◽  
NARENDRA LARIYA
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Chronic Stable Angina ◽  
Phosphate Buffer Solution ◽  
Gelling Agent ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Hydrophilic Lipophilic Balance

Objective: Aim of this study was to develop the topical delivery containing ivabradine hydrochloride (IVH) loaded transpersonal gel for symptomatic treatment of chronic stable angina pectoris in coronary artery disease. Methods: Different hydrophilic-lipophilic balance (HLB) values of surfactants-tween-80, span-80 and sodium deoxycholate (SDC) were investigated to prepare transfersomes (TFs)respectively, with different concentration of soya phosphatidylcholine and 10% v/v ethanol in phosphate buffer solution (pH 6.8) by conventional rotary evaporation sonication method. The prepared formulations were evaluated for percentage entrapment efficiency (%EE), deformability index (DI), turbidity, vesicle shape and size, in vitro drug release study and stability. SEM was done on selected formulation F8 and liposome formulation (LF). Gel was prepared by using carbopol-940 as a gelling agent with propylene glycol, polyethylene glycol solution as permeation enhancer by 32 factorial design optimization methods. The developed gel was evaluated for pH, viscosity, drug content, ex-vivo permeation studies and stability studies of TFs-gel. This was compared with LF-gel prepared by same procedure. Results: Maximum % EE (78.4±0.94), suitable vesicular size (128.6 nm) and maximum DI (34.9±1.9) was found in TFs-TW-80 and selected for gel development. In vitro drug release data from TFs-TW-80, plain drug solution and liposomal formulation (LF) revealed that % cumulative drug released in TFs-TW-80 was found maximum (89.5±0.12 %) in 20 min than others. It was 2.1 times higher than LF and 3.3 times higher than the plain drug. SEM study showed spherical shape of vesicles. The drug contents in the TFs and LF gels were found to be 92 to 95%w/w. Partition coefficient for TFs-loaded gel was 1.04±0.03. Ex vivo permeation study from hairless rat skin showed that permeation of drug is described by firstly first-order kinetics than zero-order kinetics. The drug released from TFs-gel was found to be 1.7 times higher than LF-gel and about 1.9 times higher than plain drug. Flux from TFs-gel was 2.04 times greater than LF-gel and 3.28 times more than plan drug. Stability studies indicated that suitable storage condition for developed gel was temperature 25 °C or less, where the pH, potency and therapeutic efficacy of formulations remain constant. Conclusion: Thus, transdermal route has become one of the most successful and innovative focus for research in drug delivery of IVH loaded TFs-TW-80 to increase stability and bioavailability.

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 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.

Fabrication and Characterization of Ocular Phase Transition Systems for Blepharitis: A Novel Approach

2020 ◽  
Vol 10 (1) ◽  
pp. 24-37
Author(s):  
Deepali Verma ◽  
Shreya Kaul ◽  
Neha Jain ◽  
Upendra Nagaich
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Eye Drops ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Erythromycin Estolate

Introduction: In the present research, erythromycin estolate loaded in-situ gel was formulated and evaluated for blepharitis in order to improve its therapeutic efficacy, precorneal residence time of the system and to enhance the ocular bioavailability. Material and Methods: The developed formulation was characterized by several parameters viz. FTIR, clarity, pH, gelation temperature, rheological studies, drug content, in vitro drug release studies, transcorneal permeation studies, bioadhesion studies, isotonicity and stability studies. Results: The optimized formulation exhibited non-fickian release diffusion with a sustained release of drug 82.76 ± 0.94% up to 8h and drug content 93.64%. Isotonicity revealed that the formulation was isotonic in nature and there was no shrinkage and busting of cells. Bioadhesion study was performed to check the adherence of the prepared in situ gel to the corneal surface for 4h. Ex vivo transcorneal permeation was observed to be significantly higher when compared with market eye drops. Histopathological studies were conducted to confirm the presence of normal ocular surface tissues by maintaining their morphological structures without causing damage to the tissues. The formulation was nonirritant as confirmed by the HET-CAM test. Stability studies and accelerated stability studies were conducted for 13 weeks and 26 weeks respectively and formulations were analyzed for the visual appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release and results showed no change in the formulations. Conclusion: The formulation was therapeutically efficacious, sterile, stable and provided controlled release over a period of time. The developed system could be a viable alternative to conventional eye drops for treatment of various ocular diseases.

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.

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. 

Proniosomes as Nano-Carrier for Transdermal Delivery of Atenolol Niosomal Gel

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
El-Assal M I A
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Cellulose Membrane ◽  
Order Kinetic ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Niosomal Gel ◽  
Optimum Formula

Objective of the study is to prepare Proniosomes that refers to a flexible vesicular carrier with the potential for drug administration through the transdermal route. Medthod: Proniosomes were prepared by the coacevation-phase separation technique The prepared formulations were evaluated for vesicle size, entrapment efficiency. The optimal poniosomes formula (A8) was prepared with different aqueous phase, incorporated in a gel base and studied for pH, viscosity, spredapility, stability, in vitro drug release and ex vivo permeation. Results: Niosomes formulations prepared with Span 40 and 60 have spherical and smaller Nano size. 25 mg atenolol loading has resulted 190.9 ± 15.033 nm sizes. EE% of the optimum formula prepared with distilled water was 62.11 to 92.38 .Rheological behavior showed combined shear thinning and thixotropic and gel was spreadable . Tested formulations were stable on cooling (4-8 oC) . In vitro drug release followed zero order kinetic, and gave sustained release. Release rate was significantly higher across cellulose membrane compared with rate skin. Amount of drug obtained after skin extraction was 92.6 ± 0.5% indicate enhanced permeation rate. Conclusion: All the proniosomal gel formulations were found through the acceptable range of vascular size and entrapment efficiency. Formulation A8 has been selected as an optimized therapeutic system of atenolol.

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 Design and Evaluation of Natamycin Nanocrystals Loaded In Situ Gel for Ophthalmic Administration

2021 ◽  
pp. 307-324
Author(s):  
Roshni Das ◽  
Marina Koland ◽  
S. M. Sindhoor
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Ex Vivo Permeation

Background: Natamycin belongs to a large group of naturally occurring polyene antifungal antibiotics derived from Streptomyces natalensis. Natamycin has a restrictive pharmaceutical role because of its extremely low aqueous solubility, which severely reduces the bioavailability of the drug. To improve the absorption of the drug, nanocrystals of natamycin were prepared and incorporated into in situ gel. Aim: To improve the solubility and absorption of natamycin nanocrystals by preparing nanocrystal in situ gel of natamycin for ophthalmic delivery Methodology: Natamycin nanocrystal was prepared using Sono-Precipitation method. Box-Behnken approach was employed to assess the influence of independent variables, namely concentration of stabilizer, sonication time and amplitude on particle size and zeta potential of the prepared nanocrystal. Optimized natamycin nanocrystal in situ gel formulations was characterized for various parameters like pH, viscosity, drug content, in vitro drug release and ex vivo permeation studies. Results: The optimized formulation of natamycin nanocrystal with a particle size of  293.9nm and zeta potential -14.6mV was incorporated into in situ gels. The pH triggered in situ gel was prepared using Carbopol and Hydroxypropyl methylcellulose (HPMC)., which showed clear preparation, pH of the formulation was closed to the pH of tear fluid, i.e., 7.4, viscosity showed pseudoplastic behaviour with immediate gelation remained for an extended period, and the drug content was around 99.70%. From the characterizations given above, PF-4 was optimized and evaluated for In vitro drug release showing slow and sustained release when compared to the marketed formulation and followed first-order kinetics with the diffusion-controlled mechanism. Ex vivo permeation through goat's cornea of PF-4 showed better permeation than marketed formulation. The stability studies of PF-4 showed that formulation was stable at the appropriate condition. Conclusion: Nanocrystals formulations of natamycin was successfully formulated and incorporated into in situ gels. Further in vivo studies need to be carried out for confirmation of pharmacological activity

scholarly journals Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
In Situ Gelling ◽  
Gel Transition

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

Sign in / Sign up

Export Citation Format

Share Document