Nanoliposomal Topical Formulation for Increasing Safety and Combating Microbial Drug Resistance in Leprosy

2021 ◽  
Vol 14 (6) ◽  
pp. 5708-5716
Author(s):  
Deep Patel ◽  
Deepa Patel ◽  
Dipali Talele
Keyword(s):  
Drug Resistance ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Topical Formulation ◽  
Drying Time ◽  
Microbial Drug Resistance ◽  
Dose Uniformity ◽  
Outer Membrane Permeability ◽  
Safe Approach

Nanoliposomes were prepared using solvent injection method and topical spray using simple dispersion method. The particle size and % Entrapment Efficiency were found 18.01 ± 0.21 nm and 87.71 ± 0.12% respectively. TEM studies showed that the particles were in spherical shape. Drying time, volume per spray, area of film and dose uniformity were found to be 280 ± 0.002 sec, 0.16± 0.021 ml, 155.57 ± 0.012 cm2 and 0.15± 0.0012 ml respectively which showed good spraying conditions on the affected area. Stability study shows that dapsone and chaulmoogra oil loaded nanoliposomal topical spray was stable at accelerated condition up to 1 month. The present investigation provides a safe approach by improving the outer membrane permeability to combat microbial drug resistance and increasing safety in leprosy treatment. 

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.

scholarly journals Preparation, characterization and scale-up of sesamol loaded solid lipid nanoparticles

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Transmission Electron ◽  
The Brain

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.

scholarly journals Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

2013 ◽  
Vol 63 (4) ◽  
pp. 517-529 ◽  
Author(s):  
Emrah Korkm ◽  
Evren H. Gokce ◽  
Ozgen Ozer
Keyword(s):  
Coenzyme Q10 ◽  
High Speed ◽  
Antioxidant Properties ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Scanning Calorimetry ◽  
Transmission Electron Microscopy Analysis ◽  
Solid Lipid

Abstract Coenzyme Q10 (Q10) loaded solid lipid nanoparticles (SLN) were prepared by the high speed homogenization method and incorporated into Carbopol 974P hydrogels. Compritol 888 ATO (C888) was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw80) were used as surfactant and co-surfactant. Optimum particle size with narrow distribution was obtained as 152.2 nm for blank and 142.4 nm for Q10 loaded SLNs. The overall charge of loaded SLNs was -13.7 ± 1.3 mV. Q10 entrapment efficiency was 89 % and the production yield was 94 %. Transmission electron microscopy analysis provided evidence of colloidal size, spherical shape while differential scanning calorimetry analysis confirmed recrystallization of the lipid after the preparation of SLNs. Trolox equivalent antioxidant capacity (TEAC) analysis has shown that antioxidant potential of Q10 can be protected in SLNs. Rheological characteristics demonstrated that the SLN incorporating gels were shear thinning and the mechanical strength of the gels was suitable for topical application. Diffusion studies from rat abdominal skin revealed that the delivery of Q10 was doubled in SLN incorporating gels, approximately 40 μg cm-2, in comparison with gels prepared with only Q10 (not incorporated in SLNs). As a result, it can be stated that Q10-SLN loaded gels can be successful delivery systems for carrying Q10 efficiently into the skin without losing its antioxidant properties.

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 Implementation of experimental design methodology in preparation and characterization of zolmitriptan loaded chitosan nanoparticles

2017 ◽  
Vol 6 (3) ◽  
pp. 16-22 ◽  
Author(s):  
Satish K. Mandlik ◽  
Nisharani S. Ranpise
Keyword(s):  
Statistical Analysis ◽  
Factorial Design ◽  
High Speed ◽  
Chitosan Nanoparticles ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Pharmaceutical Journal ◽  
Optimization Method ◽  
Fickian Diffusion ◽  
Contour Plots

The present study investigated the implementation of 32 factorial design of experiment and statistical analysis for the optimization of chitosan nanoparticles containing zolmitriptan an antimigraine drug. The influence of chitosan concentration (X1) and sodium tripoly phosphate (X2) on responses namely nanoparticle size (Y1), and entrapment efficiency (Y2), was studied. As per design, nine runs of nanoparticles were prepared by modified ionic gelation method using high speed vortex mixing. The particle size was found in the range of 151-880 nm and entrapment efficiency was 72.3-81.2%. A statistical analysis was performed using licensed design expert software V.8.0 with respect to ANOVA, regression analysis. The contour plots and response surface plots showed visual representation of relationship between the experimental responses and the set of independent variables. Regression model equations were validated by a numerical and graphical optimization method. Further, optimized drug loaded nanoparticles showed +23.7mV zeta potential indicating storage stability, electron micrograph reflects spherical shape and mixed type of drug release followed by Fickian diffusion (n=0.266) was observed. Thus, using systematic factorial design approach, desirable goals can be achieved in shortest possible time with lesser number of experiments which was proven to be an effective tool in quality by design.Mandlik and Ranpise, International Current Pharmaceutical Journal, February 2017, 6(3): 16-22http://www.icpjonline.com/documents/Vol6Issue3/01.pdf

scholarly journals Transcutol® P Containing SLNs for Improving 8-Methoxypsoralen Skin Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 973
Author(s):  
Giulia Pitzanti ◽  
Antonella Rosa ◽  
Mariella Nieddu ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Skin Permeability ◽  
Puva Therapy ◽  
Ultraviolet A ◽  
3T3 Fibroblasts ◽  
Skin Delivery

Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.

scholarly journals ENRICHMENT OF IN VIVO EFFICACY OF CATECHIN RICH EXTRACT WITH THE APPLICATION OF NANOTECHNOLOGY

2018 ◽  
Vol 10 (5) ◽  
pp. 281
Author(s):  
Monika P. ◽  
Basavaraj B. V. ◽  
Chidambara Murthy K. N. ◽  
Ahalya N. ◽  
Bharath S.
Keyword(s):  
Zeta Potential ◽  
Organic Solvents ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Major Elements ◽  
Oral Dosage ◽  
Biological Efficiency ◽  
Evaporation Technique ◽  
Selection Of

Objective: The primary goal of this study was to convert a natural catechin-rich extract into nanoparticles by using a biodegradable and non-toxic polymer Eudragit L 100 to address the various biopharmaceutical problems of catechin.Methods: Nanoparticles were prepared by emulsion solvent evaporation technique using Eudragit L 100 in increasing concentration. Optimization of processing conditions like a selection of organic solvents, diluent and surfactant concentrations, drug and polymer ratio and method of drying to increase the biological efficiency were duly attempted. Parameters such as dynamic light scattering, zeta potential, SEM and energy-dispersive X-ray spectroscopy were assessed for the evaluation of nanoparticles.Results: The entrapment efficiency was found to be between 35-45 % with methanol compared to other organic solvents. The zeta potential values of all the formulations were in the range of±30 mV to±60 mV) which confirms moderate to good stability. A rapid or ‘burst’ effect of the drug release in pH 6.8 buffer showing 92 % in the first 30 min which gradually decreased to 52 % by the end of 180 min but in the pH 7.4, the release was found to be moderate. SEM and DLS indicated particles were of spherical shape lying in a nanometer range of 100 to 200 nm with a proportional influence of polymer on the particles size.Conclusion: Nanoformulations were found to be more stable and confirmed the presence of major elements such as carbon and oxygen. The findings collectively indicate that it may be worthwhile to apply nanotechnology for the design of an advanced oral dosage form for an enhanced bioavailability and biological efficacy.

scholarly journals FORMULATION AND DISSOLUTION PROFILE STUDY OF TRANSFERSOME-LOADED MICROSPHERES FROM GREEN TEA LEAF EXTRACT

2018 ◽  
Vol 10 (1) ◽  
pp. 211 ◽  
Author(s):  
Effionora Anwar ◽  
Putri Amalia Handayani
Keyword(s):  
Green Tea ◽  
Leaf Extract ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Dissolution Profile ◽  
Physicochemical Stability ◽  
Span 80 ◽  
Tea Leaf ◽  
Profile Study

Objective: The aim of this study was to prepare transfersome-loaded microspheres which had good characteristics and physicochemical stability toincrease bioavailability of the polyphenol component of green tea leaf extract in the body.Methods: Transfersomes were prepared using a thin-layer hydration method. Green tea leaf extract transfersomes were formulated in the ratio of95:5, 90:10, and 85:15 based on their phospholipid and Span 80 content.Results: The most successful formula produced transfersomes of a spherical shape, 78.75 nm in size with a polydispersity index of 0.187, zetapotential of −37.5 mV, and entrapment efficiency of 47.96±5.81%. Subsequently, the transfersome was loaded into a microsphere using the spray-drymethod. The microspheres had a non-spherical, wrinkled shape, their size was 2058.44 nm, their polydispersity index was 0.545, their entrapmentefficiency was 59.27±0.59%, their moisture content was 5.21%, and their swelling index was 289.36% after 4 h. The total cumulative amount ofEpigallocatechin-3-gallate after a dissolution test was 69.15±7.66%.Conclusion: The physicochemical stability of transfersome-loaded microspheres was not significantly different from that of transfersome powder.

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