Comparative study of proniosomal drug delivery system of flurbiprofen (original) (raw)
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Formulation and Evaluation of Pronisomal Based Drug Delivery System of Flurbiprofen
………………………………………………………………………………………………………………………… Abstract: The present study on Flurbiprofen is an attempt to prepare proniosome based drug delivery system by slurry method using various non-ionic surfactants, namely span 20 (Sp 20), span 40 (Sp 40), span 60 (Sp 60) and span 80 (Sp 80) with cholesterol and spray dried lactose as carrier and to evaluate its performance. The proniosome formulation was evaluated for angle of repose, scanning electron microscopy, entrapment efficiency, In-vitro release study, Kinetic data analysis, Stability study. The result from SEM analysis has showed porous surface of proniosome. The formulation F9 which showed higher entrapment efficiency of 86.23 ± 1.34 and in-vitro release of 96.63 ± 0.24% at the end of 13 hrs was found to be best among the all twelve formulations. Release was best explained by the first order kinetics. The n value was found to be n<0.5, this revealed that the drug release follows fickian diffusion. Proniosome formulation has showed appropriate stability for 90 days by storing the formulation at accelerated stability condition.
2014
Many novel approaches bring revolutionary changes to covering various routes of administration, to achieve either controlled or targeted delivery. Proniosomes are based on dry formulation of water soluble carriers that are coated with surfactant. It forms niosomal dispersion immediately during the rehydration to before use on agitation in hot aqueous media within minutes. Proniosomes are physically stable during the storage and transport. Drug encapsulated in the vesicular structure of proniosomes prolong the existence of drug in the systematic circulation and enhances the penetration into target tissue and reduce toxicity. Due to the limited amount of water present, these systems behave as viscous phases. The various phases of liquid crystalline structures can be utilized as such for topical/transdermal applications or can be used after further hydration to form niosomes. An introduction to the skin structure along with the conversion of proniosomal gel to niosomes is also explaine...
In vitro Dynamics of Ibuprofen Incorporated Proniosomal Gel
Indian Journal Of Pharmaceutical Education And Research, 2014
The research was aimed to encapsulate the ibuprofen with proniosomal gel and facilitate ibuprofen release in sustained manner for sustained drug release. Methods: Different proniosomal gels of ibuprofen were formulated with Span 20/Span 80 and soya lecithin using the method described in literature. In all formulations cholesterol concentration was kept constant. The prepared proniosomal gels were evaluated for chemical incompatibility by FT-IR, vesicle size analysis, encapsulation efficiency, in vitro drug permeation and in vitro drug release kinetics were performed. Results: The principal absorption peaks of ibuprofen were retained in the proniosomal gels indicating that there was no interaction between ibuprofen and excipients. Vesicular diameter markedly depended on the type of the non-ionic surfactant used. As the outer diameter depends on the HLB value of surfactant, the vesicular diameter was less for proniosomes prepared using Span 80 (low HLB). The encapsulation efficiency was more for the proniosomal gels prepared using Span 20. Proniosomal gel prepared using Span 80 showed higher flux across the membrane due to its leaky membrane. The order of ibuprofen release from the proniosomal gel was PN2>PN4>PN1>PN3. Conclusion: The optimized proniosomal gel formulation PN3 containing Span 20 exhibited prolonged ibuprofen release profiles. Fickian diffusion mechanism was observed with the PN3 formulation which was due to the sustained release property. The results indicated that the proniosomal gel would be an effective transdermal delivery system for ibuprofen.
In Vitro Evaluation of Proniosomes as a Drug Carrier for Flurbiprofen
AAPS PharmSciTech, 2008
The purpose of the present investigation is to formulate and evaluate proniosomal transdermal carrier systems for flurbiprofen. Proniosomes were prepared using various non-ionic surfactants, namely span 20 (Sp 20), span 40 (Sp 40), span 60 (Sp 60) and span 80 (Sp 80) without and with cholesterol at percentages ranging from 0% to 50%. The effect of surfactant type and cholesterol content on drug release was investigated. Drug release was tested by diffusion through cellophane membrane and rabbit skin. Drug release from the prepared systems was compared to that from flurbiprofen suspensions in distilled water and HPMC (hydroxypropylmethylcellulose) gels. In case of Sp 20 and Sp 80, the added amount of cholesterol affected the preparation type to be either proniosomal alcoholic solutions or liquid crystalline gel systems. On the other hand, both Sp 40 and Sp 60 produced gel systems in presence or absence of cholesterol. Microscopic observations showed that either proniosomal solutions or gel formulations immediately converted to niosomal dispersions upon hydration. Due to the skin permeation barrier, rabbit skin showed lower drug diffusion rates compared to cellophane membrane. The proniosomal composition controlled drug diffusion rates to be either faster or slower than the prepared flurbiprofen suspensions in HPMC gels or distilled water, respectively. In conclusion, this study demonstrated the possibility of using proniosomal formulations for transdermal drug delivery.
2021
PURPOSE The objective of this study was to optimize the Flurbiprofen (FB) nanosuspension (NS) based gel and to investigate the in vitro release, ex vivo permeation, the plasma concentration-time profile and pharmacokinetic parameters. METHODS FB-NSs were developed using the wet milling process with the Design of Experiment (DoE) approach. The optimum FB-NS was characterized on the basis of SEM, DSC, XRPD, solubility and permeation studies. The dermal gel was prepared by incorporating FB-NS into HPMC gel. Then the in-vitro release, ex vivo permeation studies were performed, and pharmacokinetic studies were evaluated on rats. RESULTS The particle size, polydispersity index and zeta potential values of optimum NS were determined as 237.7 ± 6.8 nm, 0.133 ± 0.030 and - 30.4 ± 0.7 mV, respectively. By means of the surfactant content and nanosized particles of the nanosuspension, the solubility of FB was increased about 7-fold. The percentage permeated amount of FB from FB-NS gel (8.40%) w...
Formulation and Permeation Kinetic Studies of Flurbiprofen Gel
Purpose: To investigate the in vitro permeation and drug release kinetics of flurbiprofen gel. Methods: Thirteen batches (G1, G2 … G13) of flurbiprofen gels were prepared using different ratios of permeation enhancers, i.e., propylene glycol (PG) and polyethylene glycol (PEG), by response surface methodology (RSM). Viscosity, pH, spreadability, consistency and drug content of the flurbiprofen gels were measured. Permeation experiments were conducted using silicone membrane in a modified Franz diffusion cell. Permeation parameters determined include diffusion coefficient (D), Flux (J), lag time (tLag), permeation coefficient (Kp), input rate (IR) and enhancement ratio (ER). Primary skin irritation test was performed for the optimized gel, G3, using 11 human volunteers. Results: Maximum solubility (72.15 ± 0.02 mg/mL) of flurbiprofen was observed in a mixture (2:1) of methanol and water. Partition coefficient (Ko/w) was determined as logP = 3.68 ± 0.11. The gels were stable under various storage conditions, and were homogenous, crystalline and transparent. Viscosity, pH, spreadability, consistency and drug content were in the range of 150 – 178 × 102 cps, 5.42 - 5.75, 5.0 - 7.0 g.cm/s, 3.0 - 9.0 mm, and 97.99 - 99.86 %, respectively. No irritation or lesions (erythma, redness and ulceration) occurred in human volunteers over a 30-day period. The optimized formulation, G3, showed maximum flux through silicone membrane. Conclusion: PG and PEG are effective enhancers of flurbiprofen from various formulations when used in various ratios
Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen
Drug Development and Industrial Pharmacy, 2014
Solid dispersion is one of the most widely used methods to enhance the solubility and dissolution rate of poor water soluble drugs. In the present study, flurbiprofen solid dispersions were prepared using solvent evaporation method by incorporating polyethylene glycol 20000 and evaluated for solubility studies, drug-carrier compatibility studies and in vitro dissolution studies. From the solubility studies, formulations F4 were selected to prepare in the form of tablets and compared with control tablets (conventional tablets using pure drug). From the results of in vitro dissolution study, tablets containing polyethylene glycol 20000 showed almost complete drug release within the 15 min. The percent drug release in 15 min (Q15) and initial dissolution rate for formulation F4 was 99.26±1.12%, 6.62%/min. These were very much higher compared to control tablets (34.95±1.29%, 2.33%/min). The relative dissolution rate was found to be 2.84 and dissolution efficiency was found to be 57.48 and it is increased by 3.5 fold with F4 formulation compared to control tablets (17.91). From the above results, it is concluded that the formulation of solid dispersions using polyethylene glycol 20000 is a suitable approach to improve the solubility and dissolution rate of flurbiprofen.
FORMULATION AND IN -VITR0 EVALUATION OF NSAID's GEL Research Article
2012
The aim of this study was to improve the transdermal permeation of Diclofenac Soduim. Permeation studies were carried out in -vitro using Cellophane Membrane. Topical gel formulations of diclofenac sodium were prepared by using Carbopol 934, Carbopol 940, sodium carboxymethylcellulose (NaCMC), polymer as a gel-forming material that is biocompatible and biodegradable. The skin permeation enhancer on release characteristics of the diclofenac sodium from the prepared gels through a standard cellophane membrane was studied in comparison with commercially available gel formulations of diclofenac sodium. In-vitro Permeability study showed that permeation studies of Carbopol 934 and marketed gel were comparable. Tne in-vitro permeation studies by using cellophane membrane in Diffusion cell revealed good improvement of permeation characteristics of diclofenac sodium using Carbopol 940 gels as compared to the commercial gels. The permeation study enhancers such as isopropyl alcohol (IPA), Po...
ACTA Pharmaceutica Sciencia, 2018
Objective: The purpose of this study was to formulate flurbiprofen (FLB) loaded methylcellulose (MC), hydroxypropyl methylcellulose (HPMC) and Carbopol®940 (C-940) based gel formulations with the help of dispersion method for topical application. Additionally, in this study also a new ultra performance liquid chromatography method was developed for the determination of FLB, which was not previously entered into the literature. Method: FLB loaded gel formulations with the help of dispersion method for topical application and to characterize the formulations according to physical appearance, pH, rheology, drug content, dissolution study and release kinetic study with the DDSolver software program. The UPLC method developed was validated for linearity, specificity, precision, sensitivity, accuracy, range and robustness. Results: Linearity was determined to be at a concentration range of 5-50 µg.mL-1. The method developed for FLB was decided to be precise due to RSD values of <2%. Recovery of the method was satisfactory owing to <2%RSD value. The drug content was found to be in the range of 98.14-99.02% indicating the uniformity of the high drug content. At the 6th hour in dissolution study, the FLB release from gels prepared with MC, HPMC, C-940 reached 99.7%,99.5% and 87.60%, respectively. In the release kinetic tests with DDSolver, the release of gels prepared with MC and HPMC showed conformity with the weibull model, whereas the gel formulation prepared with C-940 showed a zero-order kinetics. Conclusion: According to the results, all gel formulations prepared have longer release times than the release of pure FLB.