scholarly journals Etodolac Containing Topical Niosomal Gel: Formulation Development and Evaluation

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Gyati Shilakari Asthana ◽  
Abhay Asthana ◽  
Davinder Singh ◽  
Parveen Kumar Sharma
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Formulation Development ◽  
Topical Gel ◽  
Niosomal Gel ◽  
Span 60

The present study aimed to investigate the delivery potential of Etodolac (ETD) containing topical niosomal gel. Niosomal formulations were prepared by thin film hydration method at various ratios of cholesterol and Span 60 and were evaluated with respect to particle size, shape, entrapment efficiency, and in vitro characteristics. Dicetyl phosphate (DCP) was also added in the niosomal formulation. Mean particle size of niosomal formulation was found to be in the range of 2 μm to 4 μm. Niosomal formulation N2 (1 : 1) ratio of cholesterol and surfactant displayed good entrapment efficiency (96.72%). TEM analyses showed that niosomal formulation was spherical in shape. Niosomal formulation (N2) displayed high percentage of drug release after 24 h (94.91) at (1 : 1) ratio of cholesterol : surfactant. Further selected niosomal formulation was used to formulate topical gel and was characterized with respect to its various parameters such as pH, viscosity, spreadability, ex vivo study, and in vivo potential permeation. Ex vivo study showed that niosomal gel possessed better skin permeation study than the plain topical gel. Further in vivo study revealed good inhibition of inflammation in case of topical niosomal gel than plain gel and niosomal formulation. The present study suggested that topical niosomal gel formulations provide sustained and prolonged delivery of drug.

scholarly journals FORMULATION AND OPTIMIZATION OF QUERCETIN LOADED NANOSPONGES TOPICAL GEL: EX VIVO, PHARMACODYNAMIC AND PHARMACOKINETIC STUDIES

2019 ◽  
pp. 156-165
Author(s):  
Y. SARAH SUJITHA ◽  
Y. INDIRA MUZIB
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Pharmacokinetic Studies ◽  
Topical Gel

Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug. Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies. Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation. Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

scholarly journals Serratiopeptidase Niosomal Gel with Potential in Topical Delivery

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Ujwala A. Shinde ◽  
Shivkumar S. Kanojiya
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Fourfold Increase ◽  
Surfactant Vesicles ◽  
Anti Inflammatory ◽  
Niosomal Gel

The objective of present study was to develop nonionic surfactant vesicles of proteolytic enzyme serratiopeptidase (SRP) by adapting reverse phase evaporation (REV) technique and to evaluate the viability of SRP niosomal gel in treating the topical inflammation. The feasibility of SRP niosomes by REV method using Span 40 and cholesterol has been successfully demonstrated in this investigation. The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome. The developed niosomes were characterized for morphology, particle size, and in vitro release. Niosomal gel was prepared by dispersing xanthan gum into optimized batch of SRP niosomes. Ex vivo permeation and in vivo anti-inflammatory efficacy of gel formulation were evaluated topically. SRP niosomes obtained were round in nanosize range. At Span 40 : cholesterol molar ratio 1 : 1 entrapment efficiency was maximum, that is, 54.82% ± 2.08, and showed consistent release pattern. Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer. In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

Prolonged Anti-Inflammatory Activity of Topical Melatonin by Niosomal Encapsulation

2014 ◽  
Vol 902 ◽  
pp. 70-75 ◽  
Author(s):  
Aroonsri Priprem ◽  
Vassana Netweera ◽  
Pramote Mahakunakorn ◽  
Nutjaree Pratheepawanit Johns ◽  
Jeffrey Roy Johns
Keyword(s):  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Rapid Decline ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Topical Gel ◽  
Anti Inflammatory ◽  
Average Size

Melatonin, encapsulated and non-encapsulated, in a topical gel, was comparatively investigated for its in vitro permeation and in vivo anti-inflammatory properties. An average size of the melatonin-encapsulated niosomes of 197 nm with a zeta potential of-78.8 mV and an entrapment efficiency of 92.7% was incorporated into a gel base. In vitro skin permeation of the same gel base incorporated with non-encapsulated melatonin or melatonin niosomes at 5% was comparatively evaluated through porcine skin using Franz diffusion cells and analyzed by spectroflurometry at λex 278 and λem 348 nm. From the same gel base, the permeation rate of non-encapsulated melatonin was about 2.5 times greater than that of melatonin-encapsulated niosomes. In comparison to piroxicam gel and hydrocortisone cream used as the positive controls, topical applications of melatonin and melatonin niosome gels tested in croton oil-induced ear edema in mice suggested that its anti-inflammatory activities were prolonged by the niosomal encapsulation. Similarly, analgesic effect of melatonin was prolonged by niosomal encapsulation using tail flick test in mice. Therefore, its immediate permeation through the skin was retarded by niosomal encapsulation which could also prolong its rapid decline in exerting anti-inflammatory and analgesic activities in vivo.

scholarly journals Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 465 ◽  
Author(s):  
Eman A. Mazyed ◽  
Abdelaziz E. Abdelaziz
Keyword(s):  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Ocular Delivery ◽  
Ethanol Injection ◽  
In Vitro Characterization ◽  
Span 60 ◽  
In Vivo Characterization

Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q8h) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q8h of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.

scholarly journals Development of Ritonavir Loaded Nanostructured Lipid Carriers Employing Quality By Design (QbD) As A Tool: Characterizations, Permeability, And Bioavailability Studies

2021 ◽  
Author(s):  
Vishal Gurumukhi ◽  
Sanjaykumar Bari
Keyword(s):  
Particle Size ◽  
Quality By Design ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Formulation Development ◽  
Enhanced Solubility ◽  
Formulation Variables

Abstract The objective of the present work was to optimize ritonavir (RTV) loaded nanostructured lipid carriers (NLCs) to improve bioavailability using quality by design (QbD) based technique. Risk assessment was studied using ‘cause and effect’ diagram followed by failure mode effect analysis (FMEA) to identify the effective high-risk variables for the formulation development. Quality target product profile (QTPP) and critical quality attributes (CQAs) were initially assigned for the proposed product. Central composite rotatable design (CCRD) was used to identify the individual and combined interactions of formulation variables. RTV loaded NLC (RTV-NLC) was prepared using emulsification-ultrasonication method. The effect of formulation variables like ultrasound amplitude, lipid concentration, surfactant concentration on their responses like particle size, polydispersity index (PDI), and entrapment efficiency (EE) were studied by CCRD. The optimized formulation was subjected to lyophilization to obtain dry NLCs for solid-state analysis. DSC and PXRD investigations showed RTV was molecularly dispersed in lipid matrix indicating amorphous form present in the formulation. FESEM and AFM depicted the spherical and uniform particles. The enhanced solubility and dissolution may be attributed due to the reduced particle size. The optimized NLCs showed good physical stability during storage for six months. RTV-NLC was further subjected to in vitro studies and found a successful sustained release rate of 92.37±1.03 %. The parallel artificial membrane permeability assay (PAMPA) and everted gut sac model have demonstrated the permeation enhancement of RTV. In vivo study observed the enhanced bioavailability with 2.86 fold suggesting optimized NLC successfully overcome the issue of solubility.

scholarly journals USE OF LACTIC ACID AND SPAN 80 IN THE FORMULATION OF LIPID BASED IMIQUIMOD VESICLES FOR GENITAL WARTS

2017 ◽  
Vol 9 (2) ◽  
pp. 292
Author(s):  
Saroj Jain ◽  
Anupama Diwan ◽  
Satish Sardana
Keyword(s):  
Particle Size ◽  
Lactic Acid ◽  
Zeta Potential ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Genital Warts ◽  
Formulation Development ◽  
Span 80

<p><strong>Objective: </strong>The objective of present study was formulation development of imiquimod using lactic acid and span 80 for topical delivery to cure genital warts.</p><p><strong>Methods: </strong>Lipid based vesicles (LBV) of 2% imiquimod were prepared with phospholipoin 90G, ethanol, lactic acid and span 80 using central composite design. The prepared vesicles were optimized statistically and characterized for particle size, zeta potential, percentage entrapment efficiency (% EE) and transmission electron microscopy (TEM). The optimized LBV were incorporated into gel formulation which was evaluated and compared with control gel and marketed formulation.</p><p><strong>Results: </strong>The optimized vesicles had particle size 394.8±9.6 nm, zeta potential-16.5±2.5 mV, % EE 88.27±0.45 and TEM study confirmed the formation of vesicular structure with spherical shape. The gel formulation of imiquimod vesicles showed positive results like spreadability 14.3±0.34 gcm/s, viscosity 13500±1.67 cp, consistency 6.1±0.14 mm and extrudability 16.47±0.11 g/cm<sup>2</sup>. <em>In vitro</em> permeation amount of drug was remarkably lower (10.13 %) than control (87.17 %) and marketed formulation (27.46 %). Results of retained drug for both <em>in vitro</em> as well as <em>in vivo</em> permeation study and local accumulation efficiency (4.021±0.2292) were considerably higher for LBV gel than control (0.1008±0.002513) and marketed formulation (0.8314±0.0300). To understand the mechanism of interaction between skin and vesicles, fourier transform infra-red spectroscopy studies were also done. Results of skin irritancy test and histological examination revealed biocompatible nature of formulation.</p><p><strong>Conclusion: </strong>Results of <em>in vitro </em>and <em>in vivo</em> studies indicated that this vesicle gel formulation provided efficient and site specific dermal delivery of imiquimod for cure of genital warts.</p>

Preparation and In Vivo Characterization of Niosomal Carriers of the Antidiabetic Drug Repaglinide

2015 ◽  
Vol 8 (1) ◽  
pp. 2756-2767 ◽  
Author(s):  
Shrishti Namdev ◽  
Kishore Gujar ◽  
Satish Mandlik ◽  
Preeti Jamkar
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Therapeutic Effects ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Span 60

The objective of this study is to prepare and characterise repaglinide niosomes using the Factorial Design strategy.Repaglinide is a potent second-generation oral hypoglycemic agent and has short half-life of 1 hour and oral bioavailability of 50%. Preparing Niosomal drugdelivery of repaglinide may increase its bioavailability which would lead to better therapeutic effects, reduce the frequency of dosing from twice a day to once a day and decrease side effects. The preliminary study was carried out for selection of surfactant and method of preparation based on least particle size and highest entrapment efficiency. For niosome preparation, organic solvent injection method was selected and span 60, cholesterol were selected as variable. A32 factorial design was used to optimize the effect of amounts of span 60(X1) and cholesterol (X2) which were the independent variables. Particle size (Y1) and entrapment efficiency (Y2) were the dependent variables. Relation between the dependent and independent variables were drawn out from the mathematical equations and response surface plots.Statistical analysis was performed using ANOVA which was found to be significant and quadratic equation was obtained by MLRA. The particle size was found to be in range of 144-497 nm and entrapment efficiency between 54-88%. Scanning electron microscopy indicated the spherical shape of the niosomes and formation of vesicle. Zeta potential analysis showed negatively charged surface with value of-36.7 mV. In vitro drug release profile showed that drug released fast initially followed by a slow release. In vivo pharmacokinetic study revealed that the niosomal preparation showed significant decrease in blood glucose level when compared to free repaglinide. The developed niosomal system also has potential of maintaining therapeutic level of RPG for longer period of time.Thus,the niosomes could be promising carriers for delivery ofrepaglinide with increased 

scholarly journals Design, Formulation, In-Vitro and Ex-Vivo Evaluation of Atazanavir Loaded Cubosomal Gel

2020 ◽  
Vol 11 (4) ◽  
pp. 12037-12054
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Relative Bioavailability ◽  
Transdermal Application ◽  
Study Results ◽  
Nano Formulation

In this study, Atazanavir (ATZ) was designed into the Nano formulation called cubosomes to improve its bioavailability and curtail the adverse effects by the transdermal route delivery of ATZ -loaded cubosomes. Around twenty cubosomal formulations were formulated using a Central composite factorial design. The effect of glyceryl monooleate (GMO), surfactant (Pluronic F 127), and Cetyltrimethylammonium bromide (CTAB) were studied using processes of emulsification and homogenization. Different concentrations of independent variables on particle size distribution, zeta potential, and entrapment efficiency were determined. FTIR, DSC, X-ray, and SEM, TEM results established that the drug was encapsulated in the cubosomes. The results suggested that the optimal formula exhibited a particle size of 100±7.9 - 345±6.4 nm and entrapment efficiency ranging from 61±4.6 - 93±0.8, zeta potential values ranging from -24.51 to -32.45 mV, polydispersity index values ranged from 0.35±0.01-0.54±0.02 of ATZ. The in vitro studies showed a controlled release pattern of drug release up to 24h. The ATZ cubosomal gel application on the in vivo absorption studies of the drug was studied in rats and compared with oral ATZ solution. The in vivo study results showed that the transdermal application of ATZ cubosomal gel considerably improves the absorption of drug compared to that of oral ATZ solution and found that the relative bioavailability is 4.6 times greater of oral ATZ solution. Thus it can be concluded that the ATZ cubosomal gel application via transdermal delivery route has the potential in increasing the bioavailability of the drug.

Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

2019 ◽  
Vol 10 ◽  
Author(s):  
Anjali Pandya ◽  
Rajani Athawale ◽  
Durga Puro ◽  
Geeta Bhagwat
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Degradation Products ◽  
Ex Vivo ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Rational Approach ◽  
Plga Microspheres ◽  
Long Acting

Background: The research work involves development of PLGA biodegradable microspheres loaded with dexamethasome for intraocular delivery. Objective: To design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Method: Present formulation involves the development of long acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D, L- lactide-co-glycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high pressure homogenization was used to facilitate formation of microspheres. Results: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology was observed using Field Emission Gun-Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and transretinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion: Considering the dire need for prolonged therapeutic effect in diseases of the posterior eye, an intravitreal long acting formulation was designed. Use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. Outcome from present research shows that developed microspheres would provide a long acting drug profile and reduce the frequency of administration thereby improving patient compliance.

scholarly journals FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

2019 ◽  
pp. 156-163
Author(s):  
AMOL SHETE ◽  
PRIYANKA THORAT ◽  
RAJENDRA DOIJAD ◽  
SACHIN SAJANE
Keyword(s):  
Phase Separation ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Separation Method ◽  
Gelling Agent ◽  
In Vivo Evaluation ◽  
Skin Delivery ◽  
Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

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