scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF NANO-STRUCTURED LIPID CARRIERS ENCAPSULATED TOLNAFTATE EMULGEL

2021 ◽  
Vol 12 (4) ◽  
pp. 37-43
Author(s):  
Alpana . ◽  
Sunil Khatak
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Research Work ◽  
Homogenization Method ◽  
Gelling Agent ◽  
Formulation Development ◽  
Infection Treatment ◽  
Carbopol 940 ◽  
Anti Fungal

This research work aimed to “Formulation of tolnaftate (TNF) loaded NLCs emulgel using hot homogenization method followed by ultrasonication method for topical application. The various parameters such as concentration of solid lipid (GMS), liquid lipid (Gelucire 44/14), and the concentration of gelling agent (Carbopol 940) were studied for particle size, zeta potential, %EE, and Viscosity of emulgel. The optimized formulation (F6) was found to be spherical in shape with a mean particle size of 104.8±44.30nm and zeta potential -33.0mV. The maximum % entrapment of tolnaftate in the optimized formulation was found to be 98.23±0.963. The in vitro drug release study demonstrated that the release of the drug from TNF-NLCs emulgel was shown in comparison to marketed formulation (KT5DERM) and pure TNF. Overall, the developed TNF-NLCs emulgel was considered as a potential anti-fungal nano-drug, providing a new direction to the fungal infection treatment.

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

Development and Characterization of Oral Nanosuspension Using Esomeprazole Magnesium Trihydrate

2020 ◽  
Vol 10 (6) ◽  
pp. 909-917
Author(s):  
Surya Goel ◽  
Vijay Agarwal ◽  
Monika Sachdeva
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
Research Work ◽  
In Vitro Dissolution ◽  
Top Down ◽  
Bottom Up ◽  
Poloxamer 188 ◽  
Esomeprazole Magnesium

Background: Nanosuspension has arisen as a lucrative, remunerative, as well as a potent approach to improve the solubility and dissolution rate of poorly soluble drug entities. Several challenges are still present in this technology which need more research. Objective: The prime aim of this research work is to develop, optimize and characterize the oral nanosuspension using esomeprazole magnesium trihydrate as a drug candidate. Methods: The drug nanosuspensions were prepared using both approaches; Top-down and Bottom-up as the combinational approach. Poloxamer 188 was used as a stabilizer in this study. All the important formulation variables, like concentration of stabilizers that may influence characteristics of the nanosuspensions, were optimized. Formulation screening was performed using the optimization process, and the optimized nanosuspension was evaluated for its particle size, polydispersity index, zeta potential, shape, in vitro drug release and stability. Results: For optimization of drug nanosuspension, the effect of Poloxamer 188 concentration and esomeprazole concentration was investigated and the optimal values were 0.3% w/v and 4 mg/ml, respectively. The particle size of nanosuspensions was in the range of 185 to 1048 nm with varying the zeta potential values from -11.2 to -27.5 mV. The in vitro dissolution rate of esomeprazole was increased up to 3-folds, approximately (92% in 90 min) as compared with crude esomeprazole drug (31% in 90 min) due to the decrease in particle size. Conclusion: The result indicated that the combination of top-down and bottom-up approach used for preparing the oral nanosuspension is a suitable approach for poorly aqueous soluble drug moieties like esomeprazole magnesium.

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>

scholarly journals FORMULATION AND EVALUATION OF ANTIFUNGAL NANOGEL FOR TOPICAL DRUG DELIVERY SYSTEM

2021 ◽  
pp. 127-134
Author(s):  
ANASUYA PATIL ◽  
PRANOTI KONTAMWAR
Keyword(s):  
Research Work ◽  
In Vitro Release ◽  
Gelling Agent ◽  
Release Kinetic ◽  
Topical Formulation ◽  
Ciclopirox Olamine ◽  
Carbopol 940 ◽  
Vitro Release

Objective: Ciclopirox olamine has been used as antifungal agent. It is used as topical formulation because oral route causes irritation and ulceration of GIT. In this research work, antifungal nanogel formulated to reduce size of particle, improve in-vitro release and in-vivo release. Methods: Ciclopirox olamine nanogel was prepared by homogenization technique and incorporation of gelling agent to produce nanogel. Ciclopirox olamine nanogel formulated using Carbopol 940. Results: Antigungal Nanogels (F1-F6) were subjected to FT-IR analysis and showed no interaction between the drug and excipients. The best formulation (F6) elicited the high in-vitro release of 83.42 % at 8 hours; zeta-potential and particle size, obtained values were 230 nm and -27 mV correspondingly. In-vitro release kinetic models were shown that formulation-F6 follows First-order kinetics and high regression coefficient value r2 0.9866. SEM image of the best formulation-F6 depicts that no breakage of nanogel. The differential scanning calorimetry thermogram of ciclopirox olamine was found to be 140.09.7°C. The DSC thermogram of physical mixture of carbopol 940 and Euragit-S 100 was found to be 1290C and 218 0C. DSC study of nanogel (F6) showed no interaction between drug and excipients. The best formulation-F6 was subjected to in-vivo study on mice which showed better effect in treating dermatitis. Conclusion: It would be concluded that the best formulation-F6 which elicited better in-vitro drug release and enhanced dermatitis scoring. Keywords: Ciclopirox-olamine, Eudragit-S100, Glycerol, Dermatitis, Carbopol-940, Cellophane membrane.

scholarly journals TIOCONAZOLE LOADED MUCOADHESIVE MICROSPHERES FOR THE TREATMENT OF VAGINAL CANDIDIASIS

2018 ◽  
Vol 10 (4) ◽  
pp. 80
Author(s):  
Shereen Ahmed Sabry
Keyword(s):  
Particle Size ◽  
Ethyl Cellulose ◽  
Research Work ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Vaginal Candidiasis ◽  
Fungal Activity ◽  
Mucoadhesive Polymers ◽  
Anti Fungal

Objective: The principal objective of this research work was to formulate tioconazole into mucoadhesive microspheres which were inserted into the vagina for sustaining the anti-fungal activity and protecting the liver and the kidney from the harmful drug side effects.Methods: Microspheres were prepared by the emulsion solvent evaporation method, using different ratios of the drug with either ethyl cellulose N14 or hydroxypropylmethylcellulose K100M (HPMC K100M) as mucoadhesive polymers. The formulated microspheres were evaluated for the particle size, entrapment efficiency, yield percentage, mucoadhesion strength, swelling percentage, pH, in vitro release of the drug and finally in vitro antifungal activity.Results: The optimized formulae were F3 and F6, which showed drug entrapment of 88.4±2.5 % and 97.8±1.6 %, yield percentage of 85.0±2.3% and 95.2±1.2%, mucoadhesion strength of 31.5±1.6 and 38.1±1.6 *103 dyne/cm2, swelling percentages of 143.1±1.3 and 154.2±0.8, pH of 4.7±0.1 and 4.6±0.5, and particle size of 400±3.5 µm and435±7. 8 µm respectively. F3 and F6 released about 72.8%±3.2 and 58.4%±2.7 of the drug after 8 h respectively. F3 and F6 showed a significant anti-fungal activity.Conclusion: Ethyl cellulose and hydroxyl propyl methylcellulose mucoadhesive microspheres are considered a good way to increase the duration of the anti-fungal activity of tioconazole with minimum side effects.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

Formulation and Evaluation of Nanosuspension of Simvastatin

2015 ◽  
Vol 8 (2) ◽  
pp. 2858-2873
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L Shid
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Factorial Design ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Total Drug ◽  
23 Factorial Design ◽  
Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the  preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin  (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial  design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity.

2020 ◽  
Vol 23 ◽  
Author(s):  
Gülsel Yurtdaş Kırımlıoğlu ◽  
Sinan Özer ◽  
Gülay Büyükköroğlu ◽  
Yasemin Yazan
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Spray Drying ◽  
Prolonged Release ◽  
Ocular Delivery ◽  
Corneal Permeability ◽  
Release Pattern ◽  
In Vitro Characterization ◽  
Ocular Bioavailability

Background: Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there’s a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit® RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its prolonged release to be promising for effective ocular delivery. Methods: In this study, MOX was incorporation was carried out by spray drying method aiming ocular delivery. In vitro characteristics were evaluated in detail with different methods. Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric nanoparticles by spray-drying process. Particle size, zeta potential, entrapment efficiency, particle morphology, thermal, FTIR, XRD and NMR analyses and MOX quantification using HPLC method were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated nanosized and spherical shape while in vitro release studies demonstrated modified release pattern which followed Korsmeyer-Peppas kinetic model. Following successful incorporation of MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for further studies by the reason of its better characteristics like cationic zeta potential, smaller particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERL-MOX 2 formulation remained stable for 3 months and demonstrated higher cell viability values for MOX. Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERLMOX 2 formulation has the potential of enhancing ocular bioavailability.

In Vitro Estimation of Photo-Protective Potential of Pomegranate Seed Oil and Development of a Nanoformulation

2019 ◽  
Vol 15 (1) ◽  
pp. 87-102 ◽  
Author(s):  
Surbhi Dhawan ◽  
Sanju Nanda
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Seed Oil ◽  
Topical Delivery ◽  
Inflammatory Activity ◽  
Pomegranate Seed Oil ◽  
Protective Potential ◽  
Release Studies ◽  
Pomegranate Seed

Background: Since ancient times, people have been using natural resources for photoprotection purposes. One such highly recognised natural agent is pomegranate seed oil, considered as wonder oil owing to the presence of several beneficial phytoconstituents. </P><P> Objective: The study aimed to establish the photoprotective potential of pomegranate seed oil through various in vitro and biochemical studies along with the formation of nanoemulsion, an efficient topical delivery system for the oil. </P><P> Method: Photo-protective potential of the oil was estimated by determining in vitro antioxidant and anti-inflammatory activity, total phenolic content, anti elastase, antihyaluronidase and anticollagenase activities of the oil. Ultrasonication method was used to formulate nanoemulsions. The optimisation was done following the central composite design. The characterisation was done by particle size analysis, zeta potential, polydispersity index, pH, viscosity, stability testing and transmission electron microscopy. The optimised nanoemulsion was loaded into a gel base for topical application and further release studies were carried out. </P><P> Results: The IC50 values of anti-elastase, anti-collagenase and anti-hyaluronidase were found to be 309 mg/ml, 4 mg/ml and 95 mg/ml respectively. The results of anti-oxidant and anti-inflammatory activity were also significant, which thereby established the photo-protective potential of the oil. The optimum batch 2 had particle size 83.90 nm, 0.237 PDI and -5.37 mV zeta potential. The morphology was confirmed by TEM. Batch 2 was incorporated into a gel base and release studies showed 74.12 % release within 7 hours. </P><P> Conclusion: Pomegranate seed oil possesses a potential photo-protective ability. Nanoemulsions proved to be a promising carrier for the topical delivery of the oil.

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