Optimization of Brinzolamide Loaded Microemulsion using Formulation by Design Approach: Characterization and In-vitro Evaluation

2020 ◽  
Vol 15 (1) ◽  
pp. 37-52 ◽  
Author(s):  
Riyaz Gohil ◽  
Asha Patel ◽  
Tosha Pandya ◽  
Abhay Dharamsi
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Ternary Phase Diagram ◽  
Effective Means ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Isopropyl Myristate ◽  
Ocular Delivery ◽  
Ocular Irritation

Background: The clinical application of Brinzolamide, a drug used in the treatment of glaucoma is limited due its poor aqueous solubility. Microemulsion based ocular delivery can be an effective means to improve its solubility and in turn the bioavailability. Objective: The main objective of the present work was optimization and characterization of Brinzolamide loaded microemulsion for the treatment of glaucoma. Method: The solubility of Brinzolamide in various oils and surfactants was checked in order to identify components of microemulsion. Pseudo-ternary phase diagram using Prosim software was plotted to identify microemulsion existence area. D-optimal mixture design was used for optimization of microemulsion. The optimized formulation consisted of Isopropyl myristate, Tween-80 and Transcutol-P as surfactant and co-surfactant respectively, and water. The chosen critical responses were droplet size, zeta potential, nepheloturbidimetric unit, and viscosity. Results: The selected optimal composition shows favorable features, such as droplet size (41.69 nm), Zeta potential (-9.496 mV), Viscosity (170.8 cps), Transparency (1.483 NTU) and pH (7.646) that are suitable for ocular delivery. Moreover, a prolonged drug release (78.08 % within 7 hour) was found in in-vitro experiments. By and large the formulation was found to be safe and nonirritant as proven by the ocular irritation study. Conclusion: Our study illustrated potential of Brinzolamide loaded microemulsion for ocular delivery for the treatment of glaucoma.

scholarly journals DEVELOPMENT OF MICROEMULSION FORMULATION FOR ORAL DELIVERY OF ROSUVASTATIN CALCIUM

2020 ◽  
pp. 35-39
Author(s):  
Himanshu Paliwal ◽  
Ram Singh Solanki ◽  
Chetan Singh Chauhan
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Oral Delivery ◽  
Water Solubility ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Microemulsion Formulation ◽  
Polyethylene Glycol 400 ◽  
Rosuvastatin Calcium

The purpose of conducting this study was to prepare an oral microemulsion formulation of Rosuvastatin calcium (RC) to improve its water solubility. Oil in water microemulsion was formulated using Oleic acid, Tween 80 and Polyethylene Glycol-400(PEG-400) as oil, surfactant and co-surfactant, respectively. The ideal proportion of surfactant: co-surfactant (Smix) was chosen by constructing pseudoternary diagrams. The microemulsion formulations which proved to be stable after thermodynamic stability testing were further evaluated for physical characteristics. Selected formulations were evaluated for droplet size, zeta potential, polydispersity index, viscosity and % drug content. The results were suggestive that optimized microemulsion formulation (F2) was thermodynamically stable and clear having a droplet size of 74.29 nm and zeta potential of -18.44.  In vitro dissolution study for optimized microemulsion was performed using a dialysis bag method and cumulative % drug release was determined. The result from the release study was indicative of improved solubility of Rosuvastatin calcium which may serve to boost up the oral bioavailability of drug.

scholarly journals Formulation and Characterization of Felodipine as an Oral Nanoemulsions

2021 ◽  
Vol 30 (1) ◽  
pp. 209-217
Author(s):  
Sumaya B. Hamed ◽  
Shaimaa N. Abd Alhammid
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Water Solubility ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Compatibility Study ◽  
Drug Content ◽  
Drug Molecules

            Felodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Results of characterization showed that felodipine nanoemulsion (F3) with (oleic acid 10%) ,(Smix 60% of tween80 :ethanol in a ratio of 3:1), (DDW 30%) was selected as the best formula, since it has a particle size of (17.01)nm, low PDI (0.392), zeta potential (-22.34mV), good dilution without drug precipitation , higher percent of drug content (99.098%) with  acceptable viscosity , and complete release of the drug after (45 min.) with significantly higher (P<0.05)   dissolution  rate in comparison with the pure drug powder. The selected formula (F3) subjected to further investigations as drug and excipient compatibility study by Fourier transform infrared spectroscopy (FTIR) The outcomes of the (FTIR) explain that the distinctive peaks for felodipine were not affected by other components and displayed the same functional group's band with very slight shifting. This indicates that there was no interaction between felodipine and other NE components. Therefore, these excipients were found to be compatible with felodipine. In conclusion, the NE was found to be an efficient method to enhance the dispersibility and permeatioins of drugs that have poor water solubility (lipophilic drugs).

scholarly journals Preparation and Evaluation of Topical Microemulsion System Containing Metronidazole

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Rajarshi Chakraborty ◽  
Ratul Bhowmik ◽  
Ranajit Nath ◽  
Sourav Datta ◽  
Apala Chakraborty
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Project Work ◽  
Isopropyl Myristate ◽  
Microemulsion System ◽  
Accelerated Stability ◽  
Preparation And Evaluation

Metronidazole is a synthetic nitroimidazole derived with antimicrobial and anti-inflammatory properties. The aqueous solubility of this drug is poor which results from low bioavailability. Limited effects on the removal of bacteria are shown in the local administration of plain metronidazole. The microemulsion system proves the efficacy of solubility and dissolution improvement of poorly watersoluble drugs such as metronidazole. The objective of this project work is to prepare and evaluate metronidazole containing topical water-in-oil microemulsion and to compare its effectiveness to other commercially available products. In this formulation, tween 80 is used as a surfactant and PEG 400 is used as a co-surfactant. In the oil phase, isopropyl myristate is used. Distilled water is used as the hydrophilic phase. The formulation of metronidazole containing microemulsion was evaluated for physicochemical parameters like pH, viscosity, conductivity, accelerated stability studies. In vitro release study was also performed to evaluate the release kinetics.

scholarly journals Optimization of Microemulgel for Tizanidine Hydrochloride

2020 ◽  
Vol 19 (2) ◽  
pp. 158-179
Author(s):  
Swati Jagdale ◽  
Sujata Brahmane ◽  
Anuruddha Chabukswar
Keyword(s):  
Spinal Cord ◽  
Drug Release ◽  
Zeta Potential ◽  
Ternary Phase Diagram ◽  
Ex Vivo ◽  
Research Work ◽  
Isopropyl Myristate ◽  
Globule Size ◽  
Cord Injury

Background: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis or spinal cord injury and treatment of muscle spasticity in spinal cord disease. Tizanidine hydrochloride belongs to BCS class II. It has low oral bioavailability and short halflife. Incorporating this drug in microemulgel is an excellent way to overcome problems associated with the drug. Objective: Present research work was aimed to develop and optimize a microemulsion based gel system for tizanidine hydrochloride. Methods: Screening of oil, surfactant and co-surfactant was carried out. Ternary phase diagram was constructed to obtain concentration range of components. The prepared microemulsion was evaluated for pH, globule size, zeta potential, conductivity, density and viscosity. 32 level factorial design was applied to study the effect of concentration of carbopol 934 and HPMC K15M on % cumulative drug release and viscosity of microemulgel using software Design Expert. Microemulgel was evaluated for pH, spreadability, viscosity, syneresis, drug content, bioadhesive strength, in-vitro as well as ex-vivo diffusion study. Results: Microemulsion was prepared by using isopropyl myristate as oil, tween 80 as a surfactant and transcutol P as cosurfactant. Largest transparent microemulsion region was found with Smix ratio of 1:1. FE-SEM showed globule size 28μm for batch B1 and zeta potential was -1.27mV indicating good stability of the microemulsion. Optimised batch was F6 which showed 92% drug release within 8 hours. It followed the Korsmeyer-Peppas model. Conclusion: A stable, effective and elegant microemulgel formulation, exhibiting good in-vitro and ex-vivo drug release was formulated.

Formulation and Evaluation of Lercanidipine Loaded Self-Nanoemulsifying Drug Delivery System

2018 ◽  
Vol 11 (3) ◽  
pp. 4112-4120
Author(s):  
J. Venkateswara Rao ◽  
T. Rama Mohan Reddy
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Droplet Size ◽  
Tween 80 ◽  
Water Soluble ◽  
In Vitro Drug Release ◽  
Ternary Phase Diagrams ◽  
Water Soluble Drug ◽  
Poorly Water Soluble Drug

In the present study, we sought to improve the solubility and bioavailability of lercanidipine HCl using self-nanoemulsifying drug delivery systems (SNEDDS). The extent of self-emulsification was checked with various oils with suitable surfactants and co-surfactants. The final optimized formulation contained Caproyl 90, Tween 80 and Labrosol as oil, surfactant and co-surfactant respectively. Based on lercanidipine solubility analysis, ternary phase diagrams were constructed for optimizing the system. The formulations were evaluated for FTIR studies, scanning electron microscopy (SEM), solubility, droplet size determination, zeta potential and stability studies. The droplet size was found to be 5.1 nm and Z-Average of 14.6 nm. The zeta potential of the optimized formulation (F16) was found to be -19.7 mV. In vitro drug release from SNEDDS was significantly higher than pure drug. Hence, lercanidipine SNEDDS is an optimum formulation strategy to enhance the solubility and oral bioavailability of this poorly water-soluble drug.

Development and Characterization of Water-in-Oil Microemulsion for Transdermal Delivery of Eperisone Hydrochloride

2020 ◽  
Vol 7 (1) ◽  
pp. 45-64
Author(s):  
Monika D. Kumbhar ◽  
Manisha S. Karpe ◽  
Vilasrao J. Kadam
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Droplet Size ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Tween 80 ◽  
Physical Parameters ◽  
Scanning Calorimetry ◽  
Spontaneous Emulsification

Background: Eperisone hydrochloride possesses short biological half-life due to first pass metabolism resulting in low bioavailability and short duration of response with toxic effects, ultimately limits its utilization for treatment of muscle spasm. Objective: In view of this background, current study was designed for the development of Eperisone hydrochloride-loaded microemulsion and Eperisone hydrochloride-loaded microemulsion based cream for topical delivery and compared it with conventional cream. Methods: Firstly, water-in-oil microemulsion was prepared by spontaneous emulsification method. The concentration of components was found out from existence of microemulsion region by constructing pseudoternary phase diagram. The oil was selected on the basis of drug solubility effect on the drug release, whereas surfactant and cosurfactant were screened on the basis of their efficiency to form microemulsion region. The influence of components on microemulsion formation, drug release capacity, permeation was studied by differential scanning calorimetry, X-ray diffraction, in-vitro release and ex-vivo drug permeation studies respectively. By using microemulsion, the cream was prepared for proving optimum structure for topical application. Microemulsion was evaluated for droplet size, zeta potential, pH, viscosity and conductivity. Besides the cream was characterized for pH, rheology and stability. Permeation of EPE from microemulsion across the rat skin was evaluated and compared with conventional cream. Results: The microemulsion consisting Isopropyl Myristrate/Water/Span 80:Tween 80 (50/8/42% by weight) possessed droplet size of 95.77nm, zeta potential of −5.23 mV with 7.25 pH and conductivity near to zero (<0.05mScm-1). Physical parameters of the cream were satisfactory, also 2.33-fold higher permeation and 1.57-fold higher release observed as compared to conventional cream. Conclusion: It can be concluded that Eperisone hydrochloride-loaded microemulsion and its cream is being effectively used for muscle spasticity by topical route.

scholarly journals FORMULATION DEVELOPMENT AND IN VITRO ANTIOXIDANT AND ANTIDIABETIC EVALUATION OF ERIOBOTRYA JAPONICA BASED SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM

2019 ◽  
pp. 313-319
Author(s):  
AMRIT PAL SINGH ◽  
GOPAL L. KHATIK ◽  
VIJAY MISHRA ◽  
NAVNEET KHURANA ◽  
NEHA SHARMA ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Droplet Size ◽  
Delivery System ◽  
Methanolic Extract ◽  
Tween 80 ◽  
Eriobotrya Japonica ◽  
Formulation Development

Objective: The aim of the present study was to develop and characterize self-nano emulsifying drug delivery system (SNEDDS) of methanolic extract of Eriobotrya japonica (Thunb.) Lindl. (E. japonica) leaves. Further in vitro antioxidant and antidiabetic potential of an optimized batch of SNEDDS was explored. Methods: Oil (Labrafil M 1944 CS), surfactant (Tween 80) and co-surfactant (Transcutol P) were selected on the basis of solubility of the methanolic extract. Twenty-seven batches of SNEDDS were prepared with different compositions of oil, surfactant and co-surfactant. The optimized batch was evaluated for its entrapment efficiency, droplet size, polydispersity index (PDI), zeta potential, transmission electron microscopy (TEM). Further, DPPH assay and α-amylase activity were also performed to check the antioxidant and antidiabetic potential of prepared SNEDDS. Results: The optimized design suggested that 10% of Labrafil M 1944CS, 30% of Tween 80 and 60% of Transcutol P could develop SNEDDS with 208 nm mean droplet size, 99.64% drug loading, 0.156 PDI and-6 mV zeta potential. TEM image confirmed the droplet size less than 100 nm and the spherical shape of SNEDDS. In vitro antioxidant and antidiabetic activities of SNEDDS revealed the increased efficacy as compared to that of the ascorbic acid and acarbose, respectively. Conclusion: The optimized batch of SNEDDS was found to improve the antioxidant and antidiabetic efficacy of methanolic extract of E. japonica.

scholarly journals Self-Nanoemulsifying Powder of Isotretinoin: Preparation and Characterization

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Hitesh Chavda ◽  
Jaimeen Patel ◽  
Gordhan Chavada ◽  
Shruti Dave ◽  
Ankini Patel ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Tween 80 ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Ir Studies ◽  
Emulsification Capacity ◽  
Poorly Soluble

In the present investigation an attempt was made to enhance the solubility and dissolution of poorly soluble drug, isotretinoin, by formulating self-nanoemulsifying drug delivery system (SNEDDS). Liquid SNEDDSs were prepared using Transcutol P as oil, Tween 80 as surfactant, and PEG 400 as cosurfactant. Pseudoternary phase diagrams were constructed to identify the efficient self-nanoemulsification region. The formulation with 40% oil (Transcutol P) and 60% surfactant: cosurfactant (Tween 80: PEG 400) ratio of 1 : 1 was optimized based on evaluation parameters for droplet size analysis, self-emulsification capacity, zeta potential, and in vitro drug release performance. The optimized system contains mean droplet size of 36.60 nm and zeta potential (ζ) −26.73 mV. The optimized formulation A1 was adsorbed onto Fujicalin to produce solid SNEDDS, which exhibited good flow properties and preserved the self-emulsification properties of liquid SNEDDS. The differential scanning calorimetry, FT-IR studies of solid SNEDDS revealed transformation of isotretinoin into molecularly dissolved state in the liquid SNEDDS. In vitro dissolution profiles showed that dissolution rate of ISN from solid SNEDDS was significantly greater as compared to pure drug.

scholarly journals Solubility Enhancement of Aripiprazole by Solid-Self Emulsifying Drug Delivery Systems

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Amoolya Chennuri ◽  
D. Prasanthi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Ternary Phase Diagram ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
In Vitro Drug Release ◽  
Pure Drug

Self-emulsifying drug delivery systems are a promising aptemsproach for the formulation of drug compounds with poor aqueous solubility. The main objective of this work was to formulate liquid and solid-self emulsifying drug delivery systems for poorly soluble aripiprazole. Aripiprazole is an atypical anti-psychotic drug used in the management of schizophrenia. The maximum solubility of aripiprazole was found in oleic acid (oil), Tween 80 (surfactant) and Transcutol P (co-surfactant). The L-SMEDDS were formulated in different ratios of oil: s-mix (surfactant: co-surfactant) from 1:9 to 9:1. For the formulation of stable SMEDDS, micro-emulsion region was identified by constructing pseudo-ternary phase diagram by phase titration method. The optimized F4 formulation was at the ratio of 4 (oil): 6 (s-mix). In-vitro drug release of F4 was significantly higher (99.89%) when compared to the pure drug (43.63%) in 1 hour. The F4 formulation had a droplet size of 115.9 nm and zeta potential of -24.9 mV. The pre-compression and post-compression parameters of the optimized S-SMEDDS formulation (SS1) containing Neusilin US2 as solid adsorbent were within the limits as per the official requirements of the Pharmacopoeia. SS1 formulation showed a better drug release (97% in 20 minutes) when compared to the marketed drug (59.75%) and pure drug (19.77%). In conclusion, this study illustrated that adsorption to solid carrier technique could be a useful method to prepare the solid SMEDDS tablets from liquid SMEDDS, which can enhance the solubility and improve the in-vitro drug release of aripiprazole.

scholarly journals Formulation and Evaluation of Nanoemulsion using Tazarotene and Curcumin

2021 ◽  
pp. 807-815
Author(s):  
Parmita Phaugat ◽  
Suchitra Nishal ◽  
Aparna Khansili
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Ternary Phase Diagram ◽  
In Vitro Release ◽  
Tween 80 ◽  
High Energy ◽  
Oral Route ◽  
Topical Formulation ◽  
Vitro Release

Aims: To formulate and evaluate nanoemulsion of Tazarotene and Curcumin Study Design: Ultrsonication Methods. Place and Duration of Study, Sample: Swami Dayanand Postgraduate Institute of Pharmaceuticals Sciences, University of Health Sciences, Rohtak; 2020-2021 Methodology: Oleic acid, tween 80, and propylene glycol were selected as oil, surfactant, and co-surfactant, respectively. The ratio of oil: surfactant: co-surfactant was selected based on a ternary phase diagram using the aqueous titration method. The selected ratio was employed to develop eight formulations of Tazarotene-curcumin by ultra-sonication. The formulations (F1-F8) were characterized using several physicochemical methods like pH, viscosity, particle size distribution, zeta potential, drug content, and in vitro release. The optimized formulation was selected based on the results of characterization. Results: The formulations (F1-F8) were formulated by using the ultrasonication (high energy) method. The optimized formulation possessed particle size 121, 0.382 PDI, and -20.1 zeta potential. The in vitro release of F6 was found to be 90.9 ± 3.1 at 24 hours. It also passed the thermodynamic stability tests. Conclusion: The current investigations conclude that Tazarotene-curcumin nanoemulsion can be used as an alternative to the oral route of tazarotene and is also useful in reducing the adverse effects associated with oral. The physicochemical evaluation of the formulation showed that the nanoemulsion had the necessary properties for a topical formulation.

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