scholarly journals Non-invasive drug delivery system for the delivery of protein/peptide using neem gum and its derivatives

2020 ◽  
Vol 10 (3) ◽  
pp. 5460-5465
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Drug Release Study ◽  
Weight Variation ◽  
Ex Vivo Permeation ◽  
Folding Endurance ◽  
Permeation Studies ◽  
Release Study ◽  
Ex Vivo Permeation Study

The present investigation is continuation of author’s previous work. In previous work, the author was prepared acrylamide grafted copolymer of neem gum and carboxymethylatedneem gum derivatives. Neem gum polysaccharide (NGP) and its derivatives viz. acrylamide grafted neem gum (NGP-g-Am) and carboxymethylated neem gum (CMNGP) were explored as film forming agent for transdermal delivery of protein/peptide drug (albumin). It was observed that films were not prepared at all the concentrations of NGP with a given concentration range. Studies show that film cannot be prepared using CMNGP even at ahigher concentration of polymer (2 % w/v solution). So only acrylamide grafted neem gum based film were prepared and evaluated. Transdermal films were prepared by using solvent casting method. The developed films were evaluated for various parameters such as drug content, folding endurance, thickness, weight variation, surface pH, moisture uptake, in vitro drug release study and ex-vivo permeation study. The films showed more than 300 folding endurance which demonstrated the good mechanical strength of film. It was also observed that after permeation studies small cracks were also formed in the films. Fabricated films were able to deliver drug upto 7 h. Drug release study and drug permeation studies showed that formulations followed zero order and KorsmeyerPepass model of kinetics. It can be concluded from the findings of the results that acrylamide graft copolymers of neem gum were able to deliver protein/peptide drugs through transdermal route.

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, IN VITRO AND EX VIVO CHARACTERIZATION OF MUCOADHESIVE BUCCAL TABLETS FOR ANTIHYPERTENSIVE DRUG

2018 ◽  
Vol 11 (8) ◽  
pp. 402 ◽  
Author(s):  
Himabindu Peddapalli ◽  
Vasudha Bakshi ◽  
Narender Boggula
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Surface Ph ◽  
Ex Vivo Permeation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Permeation Studies ◽  
Buccal Tablets ◽  
Pass Metabolism

Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism. Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76±0.28–6.89±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg h−1cm−2.Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

Transmucosal Delivery of Duloxetine Hydrochloride for Prolonged Release: Preparation, in vitro, ex vivo Characteri-zation and in vitro-ex vivo Correlation

2018 ◽  
Vol 11 (5) ◽  
pp. 4249-4258
Author(s):  
Nagaraj Banala ◽  
Himabindu Peddapalli ◽  
Narendar Dudhipala ◽  
Krishna Mohan Chinnala
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Content Uniformity ◽  
Prolonged Release ◽  
Duloxetine Hydrochloride ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Buccal Tablets ◽  
Transmucosal Delivery

Duloxetine hydrochloride is a selective serotonin and nor adrenaline reuptake inhibitor. It is used in the treatment of depression, diabetic peripheral neuropathic pain and in moderate to severe stress urinary incontinence in women. However, it undergoes extensive hepatic first-pass metabolism and susceptible to undergo degradation in acidic environment of stomach, which results in the poor bioavailability. The objective of the present study was to develop and evaluate the mucoadhesive buccal tablets (transmucosal delivery) of duloxetine hydrochloride with a goal of to increase the bioavailability and improve the patient compliance. Mucoadhesive buccal tablets were prepared by a wet granulation technique using mucoadhesive polymers like HPMC K4M, Carbopol 934P and PEO WSR 303. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, in vitro bioadhesion and ex vivo permeation studies. The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets AA1, AB3 and AC1 showed prolonged drug release for a period of 6 h with the Higuchi model release profile. Further, ex vivo permeation studies for optimized tablets were conducted and shown enhanced drug permeation. Therefore, these results demonstrated that the optimized buccal formulation of duloxetine hydrochloride enhances the oral bioavailability by delivered through the buccal route. 

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.

Development of Effervescent Tablets of Alendronate Sodium with Improved Intestinal Permeation

2018 ◽  
Vol 11 (1) ◽  
pp. 3990-3997
Author(s):  
Prasad Vure ◽  
Sundeep Chaurasia
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Alendronate Sodium ◽  
Drug Content ◽  
Weight Variation ◽  
Permeation Studies ◽  
Intestinal Permeation

The aim of the present study is to develop effervescent tablets of alendronate sodium to improve their intestinal permeability to treat osteoporosis. Effervescent tablets of alendronate sodium were developed with different ratios of acid to alkaline components having a pH of about 3 to about 6.5. The tablets were prepared by direct compression method. The physical mixture blend was evaluated for angle of repose, true density, bulk density, compressibility index. The formulated tablets were subjected to thickness, weight variation, hardness, friability, drug content and pH. The in vitro dissolution studies were carried out using the USP Type 2 apparatus. Formulation F14 was considered as optimized formulation because it shows drug release pattern higher than that of the other formulations and conventional marketed formulation. Ex vivo permeation studies were performed for the optimized formulation (F14) and that of the conventional marketed formulation. The drug release of the formulation (F14) was higher than the marketed formulation. Accelerated stability studies of the optimized formulation indicated that there were no signs of visually distinguishable changes, drug content and in vitro dispersion time. Thus, an increase in drug release may enhance absorption, in turn may enhance bioavailability.       

HPMA copolymer conjugate with pirarubicin: In vitro and ex vivo stability and drug release study

2018 ◽  
Vol 536 (1) ◽  
pp. 108-115 ◽  
Author(s):  
Waliul Islam ◽  
Jun Fang ◽  
Tomas Etrych ◽  
Petr Chytil ◽  
Karel Ulbrich ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Hpma Copolymer ◽  
Drug Release Study ◽  
Release Study

scholarly journals STUDYING THE EFFECT OF DIFFERENT VARIABLES ON THE FORMULATION OF MUCOADHESIVE BUCCAL PATCHES OF CAPTOPRIL

2017 ◽  
Vol 9 (2) ◽  
pp. 16
Author(s):  
Zainab Ahmed Sadeq ◽  
Nawal Ayash Rajab
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Differential Scanning Calorimetric ◽  
Content Uniformity ◽  
Weight Variation ◽  
Film Forming ◽  
Ex Vivo Permeation Study ◽  
Calorimetric Studies

Objective: The objective of this research was to formulate the captopril as mucoadhesive buccal films for hypertension treatment and studying the effect of different variables on the physical and mechanical behavior of the prepared films.Methods: The bucco-adhesive patches were prepared using hydroxyl propyl methyl cellulose K4 (HPMC) as film forming a polymer with secondary polymer included carbopol 934 and eudragit RL100. The patches were prepared by a solvent casting method and evaluated for the weight variation, surface pH, mechanical properties, content, uniformity, ex-vivo mucoadhesive strength, ex-vivo permeation study and drug release study.Results: Formula F5 containing HPMC as primary polymer with carbopol 934 as secondary polymer was chosen to be the best formulation for the following parameters: surface pH6.44, tensile strength (16.06), percentage elongation at break (34.14), swelling index(18.85), mucoadhesive strength(26.2 gm) and the folding endurance was>300 with an in vitro drug release about 94.73% during 6 h.Fourier transforms infrared spectroscopy (FT-IR) and differential scanning calorimetric studies (DSC) showed no interaction between the drug and polymers.Conclusion: It can be concluded that oral mucoadhesive buccal film of captopril, an antihypertensive agent can be prepared utilizing HPMC as a film forming a polymer with carbopol as a secondary polymer which extended the drug release through the buccal mucosa for 6 h.

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 PREPARATION AND CHARACTERIZATION OF TRIFLUOPERAZINE LOADED TRANSDERMAL PATCHES FOR SUSTAINED RELEASE

2021 ◽  
pp. 186-191
Author(s):  
ANJU PARAMBIL ◽  
SEENIVASAN PALANICHAMY ◽  
ARUL KUTTALINGAM ◽  
VELLAPANDIAN CHITRA
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Drug Loading ◽  
Polymeric Matrix ◽  
Infrared Spectroscopic Study ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Folding Endurance ◽  
Release Study

Objective: The purpose of the present study was to formulate and evaluate the polymeric transdermal delivery system of antipsychotic drug Trifluoperazine (TFP) for sustained drug release. Methods: A transdermal patch loaded with (TFP) was formulated by solvent casting technique. Polyvinyl pyrrolidone (PVP) K-30 and ethyl cellulose (EC) was used as a polymeric matrix with different ratios. Di n-butyl phthalate was used as a plasticizer. The parameters such as thickness, folding endurance and weight variation of the prepared patches were studied. The interaction study by attenuated total reflectance-infrared (ATR-IR) spectroscopy, X-ray diffraction and thermal analysis by differential scanning calorimetry (DSC) were performed. In vitro drug release study was performed by modified paddle over-disc technique. Results: The infrared spectroscopic study confirmed the absence of any chemical interaction between TFP and selected polymers. All the prepared formulations showed folding endurance values ranging from 130-162 and a satisfactory drug loading of 90-95%. In in vitro drug release study, formulations PE-3 and PE-4 exhibited a sustained and stable cumulative release of 54 % and 48% respectively, at the end of 24 h. The DSC and XRD analysis proved the partial conversion of the drug from crystalline to amorphous form when integrated into the polymeric matrix. Conclusion: The prepared transdermal formulations using polymers PVP and ethyl cellulose demonstrated their ability to sustain the release of TFP. The developed formulation could be exploited for multiday therapy of TFP for the effective treatment of schizophrenia with a simplified dosing regimen and enhanced patient compliance.

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