Formulation and in-vitro evaluation of niosomal drug delivery system for aceclofenac (original) (raw)
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Formulation and in-vitro evaluation of Niosomes of Aceclofenac
Journal of Scientific and Innovative Research
The present research work was to formulate and evaluate the site specific delivery of aceclofenac niosomes in order to overcome the problem of GI discomfort and to produce a better therapeutic response. Niosomes of Aceclofenac were formulated by an Ether injection method using different concentrations of drug, cholesterol and surfactant (Span 60). The formulations were evaluated from the various methods like vesicle shape, particle size, entrapment efficiency, drug content, compatibility studies and in-vitro drug release. Ether injection method was found to be most satisfactory with respective to niosomes particle size, drug entrapment efficiency, in-vitro drug release and its release mechanism was followed by krosmeyer Peppas method R2 =0.9840.
EVALUATION OF ACECLOFENAC NIOSOMES PREPARED BY VARIOUS TECHNIQUES Research Article
2012
The current investigation were aimed to develop sustain release formulation of aceclofenac niosomes in order to minimize gastrointestinal disturbances and to provide better therapeutic effect. Aceclofenac niosomes was prepared by different techniques namely Ether injection method (F1), Ethanol injection method (F2), Sonication method (F3), Thin film hydration (F4) and Reverse phase evaporation technique (F5) using 1:1:1 ratio of drug, cholesterol and surfactant (Span 60). The formulations were optimized from the above methods with respect to vesicle shape, particle size, entrapment efficiency, drug content, compatibility studies and in-vitro drug release. The well spherical shaped niosomes were obtained in all the methods. FT-IR Spectra shows the drug and excipients were compatible. The in-vitro release studies indicates that all the formulations exhibits retarded release for 24hrs but the thin film hydration method and reverse phase evaporation method was found to be most satisfact...
Int. J. Chem. Sci, 2014
Niosomes are non-ionic surfactant vesicles are microscopic lamellar structures formed on the admixture of non-ionic surfactant of alkyl or dialkyl polyglycerol ether class and cholesterol with subsequent hydration in aqueous media. Niosomes were formed using sorbitan esters (span 20, 40, 60 and 80) and cholesterol in different molar ratios. Acelofenac niosomes are formed using ether injection method. The so formed niosomes were evaluated for their in-vitro drug release and the best formulation with sustained drug release was formed with span-60. The mechanism of drug release was governed by peppas.
Formulation, evaluation, and in vitro drug diffusion of niosomal gel of selected drug
International journal of health sciences
Aim: To minimise toxicity and alter pharmacokinetic and bioavailability, niosomes are becoming more significant in medication delivery. Rheumatoid arthritis, juvenile rheumatoid arthritis, and degenerative joint disease may benefit from this new non-steroidal anti-inflammatory, antipyretic, and analgesic drug. Materials and Methods: Non-ionic surfactants (Span 40, 60, and Tween 60) and cholesterol were used in various ratios to create tolmetin sodium niosomes in a thin film hydration process (CHO). Evaluations of the formulations were conducted in terms of size, shape, encapsulation efficiency, and in vitro drug release. Results: In vitro drug release ranged from 94.87±0.45 to 93.19±0.45 percent in 24 hours for niosomes that looked spherical in entrapment efficiency. Incorporating Tolmetin sodium niosomes with Span 60 and CHO in the ratio of 1:2.1 into Carbopol gel was shown to be promising. Tolmetin drug noisome has a drug content and pH of 99.19±1.20 and 7.0±0.06, respectively. Co...
Design and Development of Niosomal Delivery System for Ketoprofen
Niosomes are efficient carriers for controlled drug delivery, to entrap hydrophilic drugs in the larger interior aqueous layer, whereas, lipophilic drugs in the outer lipid bilayers. Since, the niosomes are biodegradable and non toxic and hence, a good carrier for targeting of therapeutic agents at the site of interest with reduced systemic toxicity. The film formation method was used for the preparation of the niosomes due to simplicity, reproducibility and high drug entrapment efficiency. The various ratios of Surfactant (Span 60) Cholesterol and Dicetyl phosphate (DCP) were used for the preparation of the niosomes. The molar ratio of 47.5:47.5:5 was found to be most suitable in terms of niosomal size drug entrapment efficiency and in vitro drug release. The average size of niosomes was observed as 4.5 µ m with drug entrapment efficiency of 62.4%. The in vitro drug release study was carried out using dialysis membrane in Phosphate buffer saline (PBS, pH 7.4) for 24 hrs. The result showed a cumulative drug release of 98% in 8 hrs. from the free drug, against 92% drug release in 24 hrs. With optimized niosomal formulation. The optimized niosomal formulation showed a sustained action of about 16 hrs was subjected to in vivo studies (anti-inflammatory activity). This formulation was found to be more effective in reducing edema after 2 hrs as compared to the free drug.
11.Design and Development of Niosomal Delivery System for Ketoprofen
Niosomes are efficient carriers for controlled drug delivery, to entrap hydrophilic drugs in the larger interior aqueous layer, whereas, lipophilic drugs in the outer lipid bilayers. Since, the niosomes are biodegradable and non toxic and hence, a good carrier for targeting of therapeutic agents at the site of interest with reduced systemic toxicity. The film formation method was used for the preparation of the niosomes due to simplicity, reproducibility and high drug entrapment efficiency. The various ratios of Surfactant (Span 60) Cholesterol and Dicetyl phosphate (DCP) were used for the preparation of the niosomes. The molar ratio of 47.5:47.5:5 was found to be most suitable in terms of niosomal size drug entrapment efficiency and in vitro drug release. The average size of niosomes was observed as 4.5 µ m with drug entrapment efficiency of 62.4%. The in vitro drug release study was carried out using dialysis membrane in Phosphate buffer saline (PBS, pH 7.4) for 24 hrs. The result showed a cumulative drug release of 98% in 8 hrs. from the free drug, against 92% drug release in 24 hrs. With optimized niosomal formulation. The optimized niosomal formulation showed a sustained action of about 16 hrs was subjected to in vivo studies (anti-inflammatory activity). This formulation was found to be more effective in reducing edema after 2 hrs as compared to the free drug.
Evaluation of different compositions of niosomes to optimize aceclofenac transdermal delivery
asianjps.com
To optimize the composition of niosomes containing aceclofenac for transdermal application, with a view to improve permeation of drug during an extended period of time. Methods: Niosomes were prepared by thin film hydration technique. A 3 2 factorial design was utilized to study the effect of the molar ratio of drug to lipid (X 1 ) and volume of hydration medium (X 2 ) on percentage drug entrapment (PDE) and vesicle size. Selected batches of niosomes were incorporated in to carbopol gel matrix to prepare the niosomal gel formulations, which were evaluated for in-vitro release, skin permeation and in vivo studies. Results: It was evident from the derived polynomial equations and constructed contour plot, a decrease in the level of X 1 and an increase in the X 2 lead to an increase in PDE and decrease in vesicle size. The polynomial equations and contour plot predicted the levels of independent variables X 1 and X 2 (0.19 and 0.46 respectively), for maximized response of PDE with constraints on vesicle size. Each of the prepared niosomal gel formulations significantly improved (P<0.05) cumulative amount of drug permeated, steady state transdermal flux and increase in paw thickness. Among the niosomal gel formulations, NA6 (prepared at high level of X 1 and medium level of X 2 ) showed best permeation and effectiveness may be due to efficient hydration of the film and more total amount of drug entrapped. Conclusion: This study demonstrates that niosomal gel formulations may offer promise as a transdermal delivery of aceclofenac to improve efficiency and better patient compliance.
Niosomal Drug Delivery - A Comprehensive Review
Asian Journal of Pharmaceutics, 2018
Niosomes or non-ionic surfactant vesicles are microscopic lamellar structures formed on admixture of non-ionic surfactant of the alkyl or dialkyl polyglycerol ether class and cholesterol with subsequent hydration in aqueous media. They are vesicular systems similar to liposomes that can be used as carriers of amphiphilic and lipophilic drugs. The basic process of preparation is the same, i.e., hydration by aqueous phase of the lipid phase which may be either a pure surfactant or a mixture of surfactant with cholesterol. After preparing niosomal dispersion, unentrapped drug is separated by dialysis centrifugation or gel filtration. A method of in vitro release rate study includes the use of dialysis tubing. Niosomes are promising vehicle for drug delivery, and being non-ionic, it is less toxic and improves the therapeutic index of the drug by restricting its action to target cells. Niosomes are unilamellar or multilamellar vesicles formed from synthetic non-ionic surfactants. They ar...
In Vitro in Vivo Evaluation of Niosomal Formulation of Famotidine
International Journal of Pharmacy and Pharmaceutical Sciences, 2020
Objective: The present study was aimed on formulation and evaluation of famotidine loaded niosomal formulation for in vitro and in vivo pharmacokinetic behaviour. Formulating it as niosomal formulation might be quite advantageous for prolonging the duration of pharmacological action and improved bioavailability. Methods: In the present study niosomal formulations were prepared by using most documented thin film hydration technique by using various grades of surfactants (span 20, 40, 60, 80) in varying ratios with cholesterol, negative charge inducer di cetyl phosphate (DCP) and drug famotidine. Suitable preformulation studies were conducted like identification of drug, excipient and drug compatibility study. The optimized drug loaded niosomes were characterized for size and morphology, polydispersity index, zeta potential, drug entrapment, in vitro release, in vivo study and stability study. Results: The results showed that the vesicles formed were spherical in shape, size ranging b...
Journal of Pharmaceutical Research International, 2021
Background: Aceclofenac is considered to the first line drug in the symptomatic treatment of rheumatoid arthritis, osteoartheritis and ankylosing spondylitis. The successful treatment of arthritis depend on the maintenance of effective drug concentration level in the body, for which a constant and uniform supply of drug is desired. The short biological half-life (about 4 hrs) and dosing frequency more than once a day as well as (70-80%) of dose is excreted by renal transport make aceclofenac an ideal candidate for formulation of niosomal gel. Methodology: The niosomal gel of aceclofenac in order to sustain the release of aceclofenac topically, decreases the side effect of GI disturbance by maintaining the concentration of the drug in the blood and decrease the renal excretion as well as frequency of dosing. Niosomal gel was prepared by coacervation phase separation method. Preformulation studies, structural analysis, in-vitro drug release study, mechanism of drug release kinetic and...