scholarly journals INVESTIGATING THE POTENTIAL OF AN ANTIDEPRESSANT INTRANASAL MUCOADHESIVE MICROEMULSION

2018 ◽  
Vol 10 (6) ◽  
pp. 125 ◽  
Author(s):  
Gurpreet Singh ◽  
Nisha Rawat ◽  
Kirti Singh ◽  
Amita Sarwal ◽  
V. R. Sinha
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Nasal Delivery ◽  
Conductivity Measurements ◽  
Titration Method ◽  
Mucoadhesive Polymer ◽  
Biochemical Estimation ◽  
Solubility Studies ◽  
Capmul Mcm

Objective: The main aim of this study was to formulate, develop and optimized a duloxetine hydrochloride (dlx-hcl) loaded mucoadhesive microemulsion intended for intranasal administration.Methods: Established on solubility studies capmul mcm, transcutol-p, labrasol were used as oil, co-surfactant and surfactant respectively. The optimized mucoadhesive microemulsion prepared using water titration method was further characterized for particle size, polydispersity index, zeta potential and conductivity measurements followed by drug content, nasal cilio toxicity and biochemical estimation of the selected formulation.Results: All physicochemical parameters conducted, proved that dlx-hcl microemulsion was appropriate for nasal delivery. Chitosan, used as mucoadhesive polymer demonstrated enhanced retention time of the microemulsion in nasal mucosa with no signs of toxicity and epithelial damage. The particle size and zeta potential were found to be of 200 nm and-15 mV respectively considering the formulation safe for nasal delivery.Conclusion: This formulation strategy can be used as an effective targeting technique for the drugs having low bioavailability and poor brain penetration along with an effective method for the treatment long-term disease like depression.

Incorporation of micro/nanoparticles of PCL with essential oil of Cymbopogon nardus in bacterial cellulose

2018 ◽  
Vol 1 (2) ◽  
pp. 37
Author(s):  
Aline Krindges ◽  
Vanusca Dalosto Jahno ◽  
Fernando Morisso
Keyword(s):  
Particle Size ◽  
Particulate Matter ◽  
Essential Oil ◽  
Zeta Potential ◽  
Bacterial Cellulose ◽  
Culture Medium ◽  
Static Culture ◽  
Cymbopogon Nardus ◽  
Cellulose Membranes

Incorporation studies of particles in different substrates with herbal assets growing. The objective of this work was the preparation and characterization of micro/nanoparticles containing cymbopogon nardus essential oil; and the incorporation of them on bacterial cellulose. For the development of the membranes was used the static culture medium and for the preparation of micro/nanoparticles was used the nanoprecipitation methodology. The incorporation of micro/nanoparticles was performed on samples of bacterial cellulose in wet and dry form. For the characterization of micro/nanoparticles were carried out analysis of SEM, zeta potential and particle size. For the verification of the incorporation of particulate matter in cellulose, analyses were conducted of SEM and FTIR. The results showed that it is possible the production and incorporation of micro/nanoparticles containing essential oil in bacterial cellulose membranes in wet form with ethanol.

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.

Novel Simultaneous Identification of Capsaicin and It’s Quantification in Transferosome Formulation By HP-TLC Technique

2020 ◽  
Vol 17 (1) ◽  
pp. 172-183
Author(s):  
Nandanwadkar Shrikrishna Madhukar Hema ◽  
Mastiholimath Vinayak Shivamurthy ◽  
Pulija Karunakar
Keyword(s):  
Particle Size ◽  
Quality Control ◽  
Regression Analysis ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Average Recovery ◽  
Morphological Studies ◽  
Drug Entrapment Efficiency ◽  
Different Levels

Introduction: Capsaicin (8-methy-N-vanillyl-6-nonenamide), a potential analgesic derived from Capsicum annuum (Chili peppers), widely used from ancient times for its pharmacological activities such as anti-inflammatory, anti-oxidant and analgesic and provides relief from migraine and diabetes. But for obvious reasons, capsaicin cannot be administered directly. The present work was designed with a focus to comply with mandatory requirement in various pharmacopeias to know the actual content of API present in final formulations. The formulation (TS3) consisting of 3% lipid, with 4:6 ratio of the polymer and solvent, was found to be the optimized formulation, which gave the best evaluation with regard to the particle size (97.03±2.68) nm, polydispersity index (0.20±0.00), higher zeta potential (61.28±2.06) mv, morphological studies and highest drug entrapment efficiency (68.34±4.24)%. The prepared transferosome formulation was subjected to characterization by validated HP-TLC method consisting of N-Hexane: Tert- Iso-butyl-methyl ether in ratio (5:15) v/v. Linearity was performed in the range of 50-1500 ng/spot with LOD/LOQ 50 ng and 150 ng, with regression analysis (R) of 99.91%. Recovery analysis was performed at 3 different levels at 80, 100 and 120 with an average recovery of 106.97%, respectively. Till now, no analytical method has been reported, associated with the characterization of pharmaceutical nano-forms (Capsaicin), like transferosomes. Thus, the maiden validated HP-TLC method for concurrent analysis of capsaicin as API in nano-transferosome may be employed in process quality control of formulations containing the said API. Background: The irritability and adverse effects post application, leading to inflammation and neural pain at the site of administration of newly Capsaicin API and its chemical entities and marketed formulations are usually related to poor permeability, leading to drug complex reactions in the development phases or therapeutic failure along with the quantification of the same in blood plasma. However, advancement in drug formulations with the use of polymer: alcohol ratio and modernized analytical techniques for the quantification of Pharmaceutical APIs seems to be emerging and promising for overcoming pain and related inflammatory complications by formulating the APIs in Transferosome formulation with Validated HP-TLC technique being used as an effective economic and precise tool for quantitative analysis of APIs in their respective nano-forms. Objective: The study proposes a novel standardized method development and validation of pharmaceutical nanoforms with Capsaicin as API. Method: Capsaicin Transferosomes were formulated using Ultra probe sonication by utilizing different proportions of phospholipid 90G dissolved in a mixture of ethanol and propylene glycol. The formulation was subjected to Dynamic Light Scattering (DLS) technique for nano-particle analysis followed by characterization with respect to particle size, polydispersity index, zeta potential and entrapment efficiency. The morphological study of vesicles was determined using SEM and TEM. A Validated HP-TLC method for the identification and determination of Capsaicin in transferosomes formulation was performed as per the ICH guidelines. Results: The formulation gave the best evaluation for particle size (97.03±2.68) nm, polydispersity index (0.20±0.00), higher zeta potential (61.28±2.06) mv, morphological studies (SEM & TEM) and highest drug entrapment efficiency (68.34±4.24)%. DSC thermograms and FTIR spectral patterns confirmed no physical interaction by polymers with API. The prepared formulation was then characterized using HP-TLC method. The best resolution was found in NHexane: Tert-Isobutyl methyl ether in a ratio of 5:15 v/v. The Rf was found to be 0.3±0.03. Linearity was performed in a range of 50-1500 ng/spot, with regression analysis (R) of 99.91% Further, recovery analysis was done at 3 different levels as 80, 100 and 120 with an average recovery of 106.97%. The LOD/LOQ was found to be 50 and 150 ng, respectively. Precision was carried out in which % RSD was found to be precise and accurate. Conclusion: The outcomes of the present study suggested that the proposed novel formulation analyzed by Validated planar chromatographic technique (HP-TLC) for Capsaicin quantification in nanoforms may be employed as a routine quality control method for the said API in various other formulations.

Formulation and Evaluation of Atenolol Nanocrystals Using 3(2) Full Factorial Design

2020 ◽  
Vol 10 (3) ◽  
pp. 306-315
Author(s):  
Rupa Mazumder ◽  
Swarnali Das Paul
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Organic Solvent ◽  
Factorial Design ◽  
Goodness Of Fit ◽  
Production Yield ◽  
Pharmacokinetic Property ◽  
Potential Yield ◽  
Simple Method ◽  
Pure Drug

Background: Atenolol is a commonly used antihypertensive drug of class III BCS category. It suffers from the problem of poor intestinal absorption or permeability thus low bioavailability. The objective of the present study was to enhance the permeability of atenolol by using a suitable technique, which is economical and devoid of using any organic solvent. Methods: The nanocrystal technology by high-pressure homogenization was chosen for this purpose, which is a less expensive and simple method. In this technique, no organic solvent was used. The study was further aimed to characterize prepared nanocrystals in the solid state by Fourier Transform Infrared Spectroscopy (FTIR), Powder X-Ray Diffraction (PXRD) patterns, particle size, zeta potential, %yield and drug permeation study through isolated goat’s intestine. An in-vivo study was carried out to determine the pharmacokinetic property in comparison to pure drug powder using rats as experimental animals. The formulation design was optimized by a 3(2) factorial design. In these designs, two factors namely surfactant amount (X1) and speed of homogenizer (X2) were evaluated on three dependent variables namely particle size (y1), zeta potential (y2) and production yield (y3). Results: PXRD study indicated the presence of high crystal content in the prepared formulation. These nanocrystal formulations were found with a narrow size range from 125 nm to 652 nm and positive zeta potential of 16-18 mV. Optimized formulations showed almost 90% production yield. Permeability study revealed 90.88% drug release for optimized formulation in comparison to the pure drug (31.22%). The FTIR study also exposed that there was no disturbance in the principal peaks of the pure drug atenolol. This confirmed the integrity of the pure drug and its compatibility with the excipients used. A significant increase in the area under the concentration-time curve Cpmax and MRT for nanocrystals was observed in comparison to the pure drug. The higher values of the determination coefficient (R2) of all three parameters indicated the goodness of fit of the 3(2) factorial model. The factorial analysis also revealed that speed of homogenizer had a bigger effect on particle size (-0.2812), zeta potential (-0.0004) and production yield (0.0192) whereas amount of surfactant had a lesser effect on production yield (-370.4401), zeta potential (-43.3651) as well as particle size (-6169.2601). Conclusion: It is concluded that the selected method of nanocrystal formation and its further optimization by factorial design was effective to increase the solubility, as well as permeability of atenolol. Further, the systematic approach of factorial design provides rational evaluation and prediction of nanocrystals formulation on the selected limited number of smart experimentation.

scholarly journals New approach in process intensification based on subcritical water, as green solvent, in propolis oil in water nanoemulsion preparation

2021 ◽  
Vol 10 (1) ◽  
pp. 208-218
Author(s):  
Fatemeh Ghavidel ◽  
Afshin Javadi ◽  
Navideh Anarjan ◽  
Hoda Jafarizadeh-Malmiri
Keyword(s):  
Antioxidant Activity ◽  
Particle Size ◽  
Zeta Potential ◽  
Subcritical Water ◽  
Process Intensification ◽  
Processing Parameters ◽  
Bioactive Materials ◽  
Propolis Extract ◽  
High Antibacterial Activity ◽  
Oil In Water

Abstract Subcritical water was used to provide propolis oil in water (O/W) nanoemulsions. To monitor and detect the main bioactive compounds of the prepared propolis extract, gas chromatography demonstrated that there were 47 bioactive materials in the propolis extract, among which pinostrobin chalcone and pinocembrin were the two key components. Effectiveness of two processing parameters such as the amount of saponin (0.5–2.0 g) and propolis extract (0.1–0.6 g), on particle size, polydispersity index (PDI), zeta potential, and antioxidant activity of the provided nanoemulsions, was evaluated. Results demonstrated that more desirable propolis O/W nanoemulsion, with minimum particle size (144.06 nm) and PDI (0.286), and maximum zeta potential (−21.71 mV) and antioxidant activity (90.86%) were made using 0.50 g of saponin and 0.53 g of propolis extract. Further analysis revealed that the prepared nanoemulsion based on optimum processing conditions had spherical shaped propolis nanodroplets in the colloidal solution with turbidity and maximum broad absorption peak of 0.08 a.u. and 292 nm, respectively. The prepared nanoemulsion had high antibacterial activity against both selected bacteria strains namely, Staphylococcus aureus and Escherichia coli.

scholarly journals Lightening Effect of Skin Lightening Cream Containing Piper betle L. Extract in Human Volunteers

Cosmetics ◽  
2021 ◽  
Vol 8 (2) ◽  
pp. 32
Author(s):  
Sharifah Shakirah Syed Omar ◽  
Hazrina Hadi ◽  
Nadzira Mohd Hanif ◽  
Hawa Mas Azmar Ahmad ◽  
Shiow-Fern Ng
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Human Subjects ◽  
Skin Barrier ◽  
Skin Tone ◽  
In Vivo Studies ◽  
Piper Betle ◽  
Melanin Content ◽  
Skin Lightening

Hyperpigmentation affects people globally with negative psychological impacts. Piper betle L. leaf (PBL) extract has many benefits including skin lightening which may reduce hyperpigmentation. The objective of this study was to develop an effective skin-lightening cream containing PBL with ideal characteristics. A formulation of base cream and PBL cream was prepared and characterized by centrifugation, particle size and zeta potential analysis, rheological profile studies and physical properties’ observation. In vivo studies on 30 human subjects tested the effects of base and PBL cream on skin-lightening, hydration, trans-epidermal water loss (TEWL) and elasticity through weekly tests 4 weeks in duration. Base and PBL creams had a non-Newtonian property with acceptable color, odor, texture, zeta potential, particle size and showed no phase separation. The in vivo study indicated a significant reduction in melanin content and an improvement in skin tone for PBL cream but not in base cream. TEWL and elasticity also showed significant reduction for both formulations, indicating a healthier skin barrier and supple skin with consistent use, although hydration fluctuated with no significant changes. The developed PBL cream showed significant results in the reduction in melanin content and improving skin tone, which shows the formulation can confer skin-lightening effect.

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