scholarly journals FORMULATION AND EVALUATION OF NANOEMULSION FOR TOPICAL APPLICATION

2019 ◽  
Vol 9 (4-s) ◽  
pp. 370-375
Author(s):  
Neha M Shaikh ◽  
S. M. Vijayendra Swamy ◽  
NAGOBA SHIVAPPA NARSING ◽  
K B Kulkarni
Keyword(s):  
Drug Efficacy ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Tween 20 ◽  
Topical Formulation ◽  
Spontaneous Emulsification ◽  
Poor Solubility ◽  
Tinea Versicolor ◽  
Econazole Nitrate

The aim of present research is to design and develop nanoemulsion of Econazole nitrate as effective treatment for tinea versicolor fungal disease. Econazole nitrate is an imidazole antifungal agent with broad spectrum activity. It belongs to BCS class II i.e. low soluble and highly permeable drug. Due to its poor solubility, it is incompletely absorbed after oral dosing and bioavailability varies among individuals. The drug efficacy of topical formulation can be limited by instability due to its poor solubility in the vehicle and low permeability. Therefore, to overcome these problems nanoemulsions have been designed. Topical nanoemulsion containing 1 % Econazole nitrate with different oils (oleic acid), surfactant (tween 20), co-surfactant (PEG 200, PEG 400) and distilled water. Various oil-in-water nanoemulsions are prepared by the spontaneous emulsification method. The nanoemulsion formulations that passed thermodynamic stability tests were characterized for appearance, pH, FTIR, viscosity, drug content, % drug entrapment efficiency and in-vitro drug release study of Econazole nitrate determined by Franz diffusion cell and stability study.

Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

2013 ◽  
Vol 6 (2) ◽  
pp. 2058-2063
Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Antitumoral Activity ◽  
Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

Ultra-deformable Liposomes as Flexible Nanovesicular Carrier to Penetrate Versatile Drugs Transdermally

2020 ◽  
Vol 10 (1) ◽  
pp. 12-20
Author(s):  
Gaurav Tiwari ◽  
Ruchi Tiwari ◽  
Rachna Singh ◽  
Awani K. Rai
Keyword(s):  
Skin Permeation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Human Organ ◽  
Ethanol Injection ◽  
Release Studies ◽  
Junction Protein ◽  
Penetration Ability

Introduction: Transferosomes also known as ultra-deformable liposomes were introduced by Gregor Cevc in 1990. These are deformable vesicles that transport drug across the skin, which is the best route of drug delivery because skin is the largest human organ with 3 kg total weight and a surface area of 1.5-2.0 m2. Methods: Transferosomes are able to efficiently deliver low as well as high molecular weight drug across the skin in terms of quantity and depth. Various methods used for the preparation of transferosomes such as thin film hydration method, reverse phase evaporation method, vortex/sonication method, ethanol injection method and freeze thaw method. Results: The prepared transferosomal preparation will be evaluated for particle shape and size, entrapment efficiency, stability study, penetration ability and skin permeation study. In vitro release studies are to be performed using a specific dissolution medium. Conclusion: Ultra deformable liposomes can be used for delivery of different drugs e.g. analgesic, anesthetic, corticosteroids, anticancer, sex hormone, insulin, gap junction protein, and albumin.

scholarly journals SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM OF EFAVIRENZ: FORMULATION, IN VITRO EVALUATION AND CHARACTERIZATION

2019 ◽  
pp. 217-226
Author(s):  
PAMU SANDHYA
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Visual Observation ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Tween 20

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.

Fabrication of Vesicular Drug Delivery of Niosomal Topical Formulation for the Effective Treatment of Osteoarthritis

2016 ◽  
Vol 12 ◽  
pp. 1-8
Author(s):  
S. Nagalakshmi ◽  
T. Sandeep ◽  
S. Shanmuganathan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Lipid Vesicles ◽  
Tween 20 ◽  
Injection Method ◽  
Topical Gel ◽  
Release Studies

Delivery of drug through topical route, delivers most convenient and novel approach. The Skin can offer several advantages as a route of drug administration although its barrier nature makes it difficult for most drugs to penetrate in to and permeate through it. During the past decades there has been a lot of interest in lipid vesicles as a tool to improve topical drug delivery. Vesicular system such as liposomes, niosomes, ethosomes and elastic deformable vesicles provide an alternative for improved skin drug delivery. In fact vesicles can act as drug carriers controlling drug release. The Research findings were intended to develop sustained release of aceclofenac niosomes formulations in order to reduce gastrointestinal disturbances and to provide better effect when applied topically. Niosomes of aceclofenac was prepared by modified ether injection method using different ratio of surfactants (Tween 20, 40, 60 & 80) with cholesterol and drug. The developed formulations were optimized based on the high entrapment efficiency and in-vitro release studies. Optimized batch was selected and made in to topical niosomal gel using gelling agents like carbopol and sodium carboxy methyl cellulose. Formulation were evaluated for various parameters like vesicle shape, vesicle size, entrapment efficiency, drug content, compatibility studies, in-vitro release studies and stability studies. Ether injection method was found to be most satisfactory in terms of niosome particle size, drug entrapment efficiency was found to be 88.68 ±0.64 % and in-vitro release studies showed 40% of sustain drug release at the end of 8 hrs of study when compared with marketed formulation. Hence, the formulated niosomal topical gel was found to be a better alternative when compared to the marketed formulation in terms of better efficacy, bioavailability and permeation.

scholarly journals FORMULATION AND EVALUATION OF GEL CONTAINING ETHOSOMES ENTRAPPED WITH TRETINOIN

2018 ◽  
Vol 8 (5-s) ◽  
pp. 315-321
Author(s):  
Rakhi Mishra ◽  
Shradha Shende ◽  
Prabhat Kumar Jain ◽  
Vivek Jain
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Three Dimensional ◽  
Entrapment Efficiency ◽  
Brick Wall ◽  
Topical Formulation ◽  
Ir Studies ◽  
Skin Retention ◽  
Drug Solution

A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. One of the best options for successful drug delivery to the affected area of skin is the use of ethosomes which can be transported through the skin through channel-like structures. Tretinoin is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Drug loaded ethosomes had been prepared using phospholipid and ethanol, were optimized and characterized for entrapment efficiency, vesicular size, shape, In-vitro skin permeation, skin retention, drug‐membrane component interaction and stability. The ethosomal formulation having 0.5 %w/v of phospholipid and 20 %v/v of ethanol (F2) showing the greatest entrapment efficiency (80.25±0.23) with small particle size (205.40±2.31nm) was selected for further skin permeation studies. The skin permeation and skin retention studies were performed on ethosomal formulation, liposomal formulation (0.5 %w/v of phospholipid without alcohol), hydroethanolic drug solution and phosphate buffer saline (pH7.4) drug solution. Among them, ethosomal formulation showed higher cumulative percentage of drug permeation (93.36±0.45%) and 8 hours than the other formulations. Scanning electron microscopy confirmed the three dimensional nature of ethosomes. Dynamic light scattering technique proved that the ethosomes has smaller vesicular size than the liposomes prepared without alcohol. FT‐IR studies revealed no interaction between the drug and membrane components. The ethosomal vesicles were incorporated in carbopol gel base and its anti‐acne was compared with the marketed gel. Our results suggest that the ethosomes are an efficient carrier for dermal and transdermal delivery of tretinoin. Keywords: Tretinoin, Ethosomes, Diffusion, Carbopol gels, Transdermal delivery.

scholarly journals DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

2022 ◽  
pp. 156-163
Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Molar Ratios ◽  
Tween 40 ◽  
A New Technique ◽  
The Stability ◽  
Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

scholarly journals Formulation and evaluation of gas powered systems of cefdinir tablets for controlled release

2020 ◽  
Vol 10 (5) ◽  
pp. 182-187
Author(s):  
Manoj R. Chincholikar ◽  
Jagdish Rathi
Keyword(s):  
Controlled Release ◽  
Sodium Bicarbonate ◽  
Ethyl Cellulose ◽  
Guar Gum ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Magnesium Stearate ◽  
Stability Study ◽  
In Vitro Dissolution

The  present  work  is  aimed  to  formulate  Cefdinir  floating  tablets  using different  hydrophilic  and  hydrophobic  polymers  like  HPMC,  Ethyl  cellulose, Xanthum gum, guar gum and gas generating agent Sodium bicarbonate. The develop gastro retentive dosage form thatcould  retain  the  agent  namely  Cefdinir  in  the  stomach  for  longer periods of time delivering the drug to the site of action, i.e., stomach. HPMC  is  used  as  a  swelling  agent,  Guar  gum  and  Xanthum  gum  is used as binding agent. Ethyl cellulose is used as matrix form agent.  PVP is used as a suspending agent. Sodium bicarbonate is used as a gas forming agent. MCC is used as a disintergrant and diluent. Magnesium stearate is used as a lubricant. The  prepared  Cefdinir  tablets  will  be  evaluated  for  drug  content,  entrapment efficiency, post compression studies, In-vitro buoyancy studies, swelling index studies, in-vitro dissolution studies, release kinetics, stability studies.All these parameters were found to be within the pharmacopoeial limits. Formulation F5 was selected for drug release and stability study on the basis of appropriate results of post compression study.In vitro dissolution study was carried out and showed controlled release pattern. Keywords: Gas Powered Systems, Cefdinir, Controlled release, Floating drug delivery.

FORMULATION AND OPTIMIZATION OF TOPICAL NANOEMULSION BASED GEL OF MOMETASONE FUROATE USING 32 FULL FACTORIAL DESIGN

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 19-29
Author(s):  
Bhupendra G. Prajapati ◽  
◽  
Malay Jivani ◽  
Himanshu Paliwal ◽  
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Tween 80 ◽  
Stability Study ◽  
Mometasone Furoate ◽  
Gelling Agent ◽  
Topical Formulation ◽  
Topical Gel

Mometasone furoate (MF) is a glucocorticoid prodrug that faces the problem of poor aqueous solubility. Nanoemulsion-based topical gel of MF was formulated to enhance its solubility and potential of treating skin conditions. The selection of oil, surfactant and co-surfactant was done based on their solubility with the drug. The nanoemulsion was prepared using rose oil as the oil phase. Tween 80 and Transcutol P were used as surfactant and co-surfactant and they were blended in different ratios (1:0, 1:1, 2:1 and 3:1 w/w). The pseudo ternary diagrams were developed using these excipients and formulations exhibiting considerable nanoemulsion region were selected. The formulations were optimized by using Design Expert software for the globule size and cumulative percent release. The nanoemulsion formulations were characterized for in vitro release and stability study. The optimized nanoemulsions consisting of 2 % w/w oil, 30 % w/w Smix (Surfactant: Co-surfactant) and 67.9 % w/w water were consolidated into Carbopol 940 gelling agent to prepare three nanoemulsion-based gel formulations or nanoemulgels (NEG1-NEG3). Nanoemulgels were evaluated for their stability and ex vivo permeation of MF. The outcomes suggested that skin permeation of MF from all the nanoemulgel formulations was significantly enhanced as compared to the marketed mometasone furoate topical formulation.

scholarly journals Development and Evaluation of Liposomes for Topical Delivery of Tacrolimus (Fk-506)

2010 ◽  
Vol 2 (3) ◽  
pp. 585 ◽  
Author(s):  
S. S. Patel ◽  
M. S. Patel ◽  
S. Salampure ◽  
B. Vishwanath ◽  
N. M. Patel
Keyword(s):  
Contact Dermatitis ◽  
Allergic Contact Dermatitis ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Stability Study ◽  
Multilamellar Vesicle ◽  
Cholesterol Ratio ◽  
Acd Model ◽  
Allergic Contact

In the present work Tacrolimus loaded liposomal systems were developed and evaluated for their topical delivery. Neutral multilamellar liposomes (MLVs) were prepared by thin film hydration method. The amount of drug loaded into vesicles ranged from 4.4 mg per 115mg to 8.2mg per 140mg of total lipid. Entrapment efficiency of tacrolimus in liposomes was studied by altering the amount of cholesterol ratio to lipid ratio. After performing stability study at different temperatures (4, 25, and 37°C) was affirms that drug leakage increased at higher temperature. The in-vitro permeation study shows significant reduced permeation with tacrolimus liposomes compared with free tacrolimus in propylene glycol. The animal study carried out on allergic contact dermatitis (ACD) model in rats showed that 0.03% tacrolimus liposomal gel exhibited similar activity when compared with 0.03% marketed tacrolimus ointment. It is also likely that tacrolimus liposomal gel which leads no visible or palpable residue when applied on skin would be more appealing to patients than conventional ointment. Overall study suggests that tacrolimus can be effectively incorporated in liposomes and can be used for the treatment of atopic dermatitis.  Keywords: Tacrolimus; Multilamellar vesicle; Allergic contact dermatitis.   © 2010 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved. DOI: 10.3329/jsr.v2i3.3258               J. Sci. Res. 2 (3), 587-598  (2010) 

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