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1.
Hydroxyzine HCl is used in oral formulations for the treatment of urticaria and atopic dermatitis. Dizziness, blurred vision,
and anticholinergic responses, represent the most common side effects. It has been shown that controlled release of the drug
from a delivery system to the skin could reduce the side effects while reducing percutaneous absorption. Therefore, the aim
of the present study was to produce an effective drug-loaded dosage form that is able to control the release of hydroxyzine
hydrochloride into the skin. The Microsponge Delivery System is a unique technology for the controlled release of topical
agents, and it consists of porous polymeric microspheres, typically 10–50 μm in diameter, loaded with active agents. Eudragit
RS-100 microsponges of the drug were prepared by the oil in an oil emulsion solvent diffusion method using acetone as dispersing
solvent and liquid paraffin as the continuous medium. Magnesium stearate was added to the dispersed phase to prevent flocculation
of Eudragit RS-100 microsponges. Pore inducers such as sucrose and pregelatinized starch were used to enhance the rate of
drug release. Microsponges of nearly 98% encapsulation efficiency and 60–70% porosity were produced. The pharmacodynamic effect
of the chosen preparation was tested on the shaved back of histamine-sensitized rabbits. Histopathological studies were driven
for the detection of the healing of inflamed tissues. 相似文献
2.
The goal of the present study was to develop and evaluate microsponge-based topical delivery system of mupirocin for sustained
release and enhanced drug deposition in the skin. Microsponges containing mupirocin were prepared by an emulsion solvent diffusion
method. The effect of formulation and process variables such as internal phase volume and stirring speed on the physical characteristics
of microsponges were examined on optimized drug/polymer ratio by 32 factorial design. The optimized microsponges were incorporated into an emulgel base. In vitro drug release, ex vivo drug deposition, and in vivo antibacterial activity of mupirocin-loaded formulations were studied. Developed microsponges were spherical and porous, and
there was no interaction between drug and polymer molecules. Emulgels containing microsponges showed desired physical properties.
Drug release through cellulose dialysis membrane showed diffusion-controlled release pattern and drug deposition studies using
rat abdominal skin exhibited significant retention of active in skin from microsponge-based formulations by 24 h. The optimized
formulations were stable and nonirritant to skin as demonstrated by Draize patch test. Microsponges-based emulgel formulations
showed prolonged efficacy in mouse surgical wound model infected with S. aureus. Mupirocin was stable in topical emulgel formulations and showed enhanced retention in the skin indicating better potential
of the delivery system for treatment of primary and secondary skin infections, such as impetigo, eczema, and atopic dermatitis. 相似文献
3.
Long Mo Guijing Lu Xiping Ou Dongsheng Ouyang 《Saudi Journal of Biological Sciences》2022,29(1):266-272
The main aim of this study is to optimize and evaluate transdermal patch of Carvedilol by the use of different polymer and different permeation enhancers which help to release drug in controlled action and thereby increase the bioavailability of the drug. Main objective was to avoid first pass metabolism of Carvedilol. Transdermal patches were developed by solvent evaporation method. The combination of Eudragit RS-100 as rate controlling polymer and Span 80 as a permeation enhancer was found to be ideal formulation (Formulation F7) with maximum drug release i.e. 100.29 ± 0.44 % within 12 h. Formulation F7 showed maximum bioavailability and showed maximum drop of BP at 6 h. From this study the conclusion was, transdermal patch of Carvedilol which contains Eudragit RS-100 polymer and Span 80 as penetration enhancer produced sustained and continued drug release. 相似文献
4.
Sha-Sha Li Guo-Feng Li Li Liu Xiao Jiang Bin Zhang Zhi-Gang Liu Xue-Ling Li Li-Dong Weng Ting Zuo Qiang Liu 《PloS one》2013,8(11)
The aim of the present study was to design a novel topical skin-target drug-delivery system, the paeonol microsponge, and to investigate its drug-release patterns in dosage form, both in vitro and in vivo. Paeonol microsponges were prepared using the quasi-emulsion solvent-diffusion method. In vitro release studies were carried out using Franz diffusion cells, while in vivo studies were investigated by microdialysis after the paeonol microsponges were incorporated into a cream base. In vitro release studies showed that the drug delivered via microsponges increased the paeonol permeation rate. Ex vivo drug-deposition studies showed that the microsponge formulation improved drug residence in skin. In addition, in vivo microdialysis showed that the values for the area under the concentration versus time curve (AUC) for the paeonol microsponge cream was much higher than that of paeonol cream without microsponges. Maximum time (Tmax) was 220 min for paeonol microsponge cream and 480 min for paeonol cream, while the half-life (t1/2) of paeonol microsponge cream (935.1 min) was almost twice that of paeonol cream (548.6 min) in the skin (n = 3). Meanwhile, in the plasma, the AUC value for paeonol microsponge cream was half that of the paeonol cream. Based on these results, paeonol-loaded microsponge formulations could be a better alternative for treating skin disease, as the formulation increases drug bioavailability by lengthening the time of drug residence in the skin and should reduce side-effects because of the lower levels of paeonol moving into the circulation. 相似文献
5.
Studies on Mefenamic Acid Microparticles: Formulation, In Vitro Release, and In Situ Studies in Rats
Ferhan Sevgi Aysu Yurdasiper Buket Kaynarsoy Ezgi Turunç Tamer Güneri Ayfer Yalçın 《AAPS PharmSciTech》2009,10(1):104-112
In this study, we investigated the in vitro characteristics of mefenamic acid (MA) microparticles as well as their effects on DNA damage. MA-loaded chitosan and alginate
beads were prepared by the ionotropic gelation process. Microsponges containing MA and Eudragit RS 100 were prepared by quasi-emulsion
solvent diffusion method. The microparticles were characterized in terms of particle size, surface morphology, encapsulation
efficiency, and in vitro release profiles. Most of the formulation variables manifested an influence on the physical characteristics of the microparticles
at varying degrees. We also studied the effects of MA, MA-loaded microparticles, and three different polymers on rat brain
cortex DNA damage. Our results showed that DNA damage was higher in MA-loaded Eudragit microsponges than MA-loaded biodegradable
chitosan or alginate microparticles. 相似文献
6.
The aim of this work was to understand the influence of different formulation variables on the optimization of pH-dependent,
colon-targeted, sustained-release mesalamine microspheres prepared by O/O emulsion solvent evaporation method, employing pH-dependent
Eudragit S and hydrophobic pH-independent ethylcellulose polymers. Formulation variables studied included concentration of
Eudragit S in the internal phase and the ratios between; internal to external phase, drug to Eudragit S and Eudragit S to
ethylcellulose to mesalamine. Prepared microspheres were evaluated by carrying out in vitro release studies and determination of particle size, production yield, and encapsulation efficiency. In addition, morphology
of microspheres was examined using optical and scanning electron microscopy. Emulsion solvent evaporation method was found
to be sensitive to the studied formulation variables. Particle size and encapsulation efficiency increased by increasing Eudragit
S concentration in the internal phase, ratio of internal to external phase, and ratio of Eudragit S to the drug. Employing
Eudragit S alone in preparation of the microspheres is only successful in forming acid-resistant microspheres with pulsatile
release pattern at high pH. Eudragit S and ethylcellulose blend microspheres were able to control release under acidic condition
and to extend drug release at high pH. The stability studies carried out at 40°C/75% RH for 6 months proved the stability
of the optimized formulation. From the results of this investigation, microencapsulation of mesalamine in microspheres using
blend of Eudragit S and ethylcellulose could constitute a promising approach for site-specific and controlled delivery of
drug in colon. 相似文献
7.
M. Maghsoodi 《AAPS PharmSciTech》2009,10(1):120-128
Microparticles of naproxen with Eudragit L100 and Aerosil were prepared by the emulsion solvent diffusion method in order
to avoid local gastrointestinal irritation, one of the major side effects of nonsteroidal anti-inflammatory drugs after oral
ingestion. The process of preparation involved the use of ethanol as good solvent, dichloromethane as a bridging liquid, water
as poor solvent, Aerosil as anti-adhesion agent, and sodium dodecyl sulfate to aid in the dispersion of the drug and excipients
into the poor solvent. The obtained microparticles were evaluated for micromeritic properties, yield, encapsulation efficiency,
drug physical state, and drug release properties. The influence of formulation factors and preparation condition (polymer/naproxen
ratio, Aerosil/polymer ratio, and the initial difference of temperature between the solvent and nonsolvent) on the properties
of the microparticles were also examined. The resultant microparticles were finely spherical and uniform with high incorporation
efficiency (>79%) and yield (>71%). The incorporation efficiency was enhanced with increasing the ratio of excipients to drug
and the initial difference of temperature between the solvent and nonsolvent. The mean diameter of the microparticles was
influenced by all of the manufacturing parameters. Studies carried out to characterize the micromeritic properties of formulations,
such as flowability and packability, showed that microparticles were suitable for further pharmaceutical manipulation (e.g.,
capsule filling). Drug release studies of the microparticles confirmed the gastroresistance, and mathematical studies showed
that the drug released followed a Hixon and Crowell kinetic. These microparticles represent a simple method for the preparation
of drug-loaded enteric microparticles with desired micromeritic properties and gastroresistance release. 相似文献
8.
The objective of the present study was to develop once-daily sustained-release matrix tablets of nicorandil, a novel potassium
channel opener used in cardiovascular diseases. The tablets were prepared by the wet granulation method. Ethanolic solutions
of ethylcellulose (EC), Eudragit RL-100, Eudragit RS-100, and polyvinylpyrrolidone were used as granulating agents along with
hydrophilic matrix materials like hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose, and sodium alginate.
The granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The
tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, and in vitro release
studies. The granules showed satisfactory flow properties, compressibility, and drug content. All the tablet formulations
showed acceptable pharmacotechnical properties and complied with in-house specifications for tested parameters. According
to the theoretical release profile calculation, a oncedaily sustained-release formulation should release 5.92 mg of nicorandil
in 1 hour, like conventional tablets, and 3.21 mg per hour up to 24 hours. The results of dissolution studies indicated that
formulation F-I (drug-to-HPMC, 1∶4; ethanol as granulating agent) could extend the drug release up to 24 hours. In the further
formulation development process, F-IX (drug-to-HPMC, 1∶4; EC 4% wt/vol as granulating agent), the most successful formulation
of the study, exhibited satisfactory drug release in the initial hours, and the total release pattern was very close to the
theoretical release profile. All the formulations (except F-IX) exhibited diffusion-dominated drug release. The mechanism
of drug release from F-IX was diffusion coupled with erosion. 相似文献
9.
Microparticulate drug delivery systems have shown a great interest in the pharmaceutical area. They allow the increase of drug therapeutic efficacy and the reduction of side effects. In this context, microsponges represent a new model of porous polymer microspheres, which allow the entrapment of a wide range of active agents. During the development, it is necessary the characterization of the system and among of the most important tests are the release and permeation profile analysis. They can demonstrate the behavior of drug in a specific site with a particular application condition and are related to therapeutic efficacy. Therefore, this review provides an overview of drug delivery profile from microsponges. Methods for determination of in vitro release and ex vivo permeation studies are detailed. Examples of drug delivery from microsponges administered in different sites are also discussed with aim to provide an understanding of the use of this strategy to modify the drug delivery. 相似文献
10.
Interpolyelectrolyte (IPE) complexation between carrageenan (CG) and Eudragit E (EE) was studied in 0.1 M HCl and was used
to develop floating matrix tablets aimed to prolong gastric-residence time and sustain delivery of the loaded drug. The optimum
EE/CG IPE complexation weight ratio (0.6) was determined in 0.1 M HCl using apparent viscosity measurements. The IPE complex
was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. Metronidazole matrix tablets
were prepared by direct compression using EE, CG, or hybrid EE/CG with ratio optimal for IPE complexation. Corresponding effervescent
tablets were prepared by including Na bicarbonate as an effervescent agent. Tablets were evaluated for in vitro buoyancy and drug release in 0.1 M HCl. Both CG and EE–CG effervescent matrices (1:2 drug to polymer weight ratio, 60 mg
Na bicarbonate) achieved fast and prolonged floating with floating lag times less than 30 s and floating duration of more
than 10 h. The corresponding EE effervescent matrices showed delayed floating and rapid drug release, and completely dissolved
after 3 h of dissolution. CG matrices showed an initial burst drug release (48.3 ± 5.0% at 1 h) followed by slow drug release
over 8 h. EE–CG matrices exhibited sustained drug release in almost zero-order manner for 10 h (68.2 ± 6.6%). The dissolution
data of these matrices were fitted to different dissolution models. It was found that drug release followed zero-order kinetics
and was controlled by the superposition of the diffusion and erosion. 相似文献
11.
The purpose of this research was to develop a matrix-type transdermal therapeutic system containing carvedilol with different
ratios of hydrophilic and hydrophobic polymeric combinations by the solvent evaporation technique. The physicochemical compatibility
of the drug and the polymers was studied by infrared spectroscopy and differential scanning calorimetry. The results suggested
no physicochemical incompatibility between the drug and the polymers. In vitro permeation studies were performed by using
Franz diffusion cells. The results followed Higuchi kinetics (r=0.9953−0.9979), and the mechanism of release was diffusion mediated. Based on physicochemical and in vitro skin permeation
studies, patches coded as F3 (ethyl cellulose: polyvinylpyr-rolidone, 7.5∶2.5) and F6 (Eudragit RL:Eudragit RS, 8∶2) were
chosen for further in vivo studies. The bioavailability studies in rats indicated that the carvedilol transdermal patches
provided steady-state plasma concentrations with minimal fluctuations and improved bioavailability of 71% (for F3) and 62%
(for F6) in comparison with oral administration. The antihypertensive activity of the patches in comparison with that of oral
carvedilol was studied using methyl prednisolone acetate—induced hypertensive rats. It was observed that both the patches
significantly controlled hypertension from the first hour (P<.05). The developed transdermal patches increase the efficacy of carvedilol for the therapy of hypertension.
Published; January 19, 2007 相似文献
12.
The release of verapamil hydrochloride from tablets with Eudragit RLPO or Kollidon®SR with different drug-to-polymer ratios were investigated with a view to develop twice-daily sustained-release dosage form by solid dispersion (SD) technique. The SDs containing Eudragit RLPO or Kollidon®SR at drug-polymer ratios of 1:1, 1:2, and 1:3 with verapamil hydrochloride were developed using solvent evaporation technique. The physical mixtures of drug and both polymers were prepared by using simple mixing technique at the same ratio as solid dispersion. The physicochemical properties of solid dispersion were evaluated by using Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The study of DSC, XRD, and FTIR could not show significant interaction between verapamil HCl and Kollidon®SR or Eudragit RLPO. The solid dispersions or physical mixtures were compressed to tablets. The tablets were prepared with solid dispersions containing Eudragit RLPO or Kollidon®SR, with all the official requirements of tablet dosage forms fulfilled. Tablets prepared were evaluated for the release of verapamil hydrochloride over a period of 12 h in pH 6.8 phosphate buffer using US Pharmacopoeia type II dissolution apparatus. The in vitro drug release study revealed that the tablet containing Eudragit has extended the release rate for 12 h whereas the tablet containing Kollidon®SR at the same concentration has extended the release rate up to 8 h. The in vitro release profile and the mathematical models indicate that release of verapamil hydrochloride can be effectively controlled from a tablet containing solid dispersions of Eudragit RLPO. The reduction of size fraction of the SD system from 200–250 to 75–125 μm had a great effect on the drug release. 相似文献
13.
Influence of selected formulation variables on the preparation of enzyme-entrapped eudragit S100 microspheres 总被引:1,自引:0,他引:1
The aim of this work is to study the influence of formulation parameters in the preparation of sustained release enzyme-loaded Eudragit S100 microspheres by emulsion solvent diffusion technique. A 3(2) full factorial experiment was designed to study the effects of the amount of solvent (dichloromethane) and stabilizers (Tween 20, 40, or 80) on the drug content and microsphere size. The results of analysis of variance test for both effects indicated that the test is significant. The effect of amount of stabilizer was found to be higher on both responses (SS(Y1) = 45.60; SS(Y2) = 737.93), whereas solvent concentration comparatively produced significant effect on the size of microspheres (SS(Y1) = 0.81; SS(Y2) = 358.83). Scanning electron microscopy of microspheres with maximum drug content (2.5 mL dichloromethane and 0.1 mL Tween 80) demonstrated smooth surface spherical particles with mean diameter of 56.83 +/- 2.88 microm. The effect of formulation variables on the integrity of enzyme was confirmed by in vitro proteolytic activity. The enteric nature of microspheres was evaluated and results demonstrated ~6% to 7% release of enzyme in acidic medium. The release of enzyme from microspheres followed Higuchi kinetics. In phosphate buffer, microspheres showed an initial burst release of 20.34% +/- 2.35% in 1 hour with additional 58.79% +/- 4.32% release in the next 5 hours. Three dimensional response graphs were presented to visualize the effect of independent variables on the chosen response. Thus, Eudragit S100 microspheres can be successfully prepared for oral delivery of enzymes with desirable characters in terms of maximum loading and diffusion release pattern. 相似文献
14.
The objective of this study was to develop a solid dispersion based controlled release system for drug substances that are poorly soluble in water. A wax-based disintegration mediated controlled release system was designed based on the fact that an amorphous drug can crystallize out from hydrophilic matrices. For this study, cilostazol (CIL) was selected as the model drug, as it exhibits poor aqueous solubility. An amorphous solid dispersion was prepared to assist the drug to attain a supersaturated state. Povidone was used as carrier for solid dispersion (spray drying technique), hydrogenated vegetable oil (HVO) as wax matrix former, and sodium carboxymethyl cellulose (NaCMC) as a disintegrant. The extreme vertices mixture design (EVMD) was applied to optimize the designed and developed composition. The optimized formulation provided a dissolution pattern which was equivalent to the predicted curve, ascertaining that the optimal formulation could be accomplished with EVMD. The release profile of CIL was described by the Higuchi’s model better than zero-order, first-order, and Hixson-Crowell’s model, which indicated that the supersaturation state of CIL dominated to allow drug release by diffusion rather than disintegration regulated release as is generally observed by Hixson-Crowell’s model. The optimized composition was evaluated for disintegration, dissolution, XRD, and stability studies. It was found that the amorphous state as well as the dissolution profile of CIL was maintained under the accelerated conditions of 40°C/75% RH for 6 months.KEY WORDS: cilostazol, controlled release, disintegration-mediated controlled release (DMCR), extreme vertices mixture design (EVMD), solid dispersion 相似文献
15.
Mani Ganesh Udhumansha Ubaidulla Pushparaj Hemalatha Mei Mei Peng Hyun Tae Jang 《AAPS PharmSciTech》2015,16(4):944-951
This study investigated the potential use of mesoporous silica nanoparticles (MSNs) as a carrier for duloxetine hydrochloride (DX), which is prone to acid degradation. Sol–gel and solvothermal methods were used to synthesize the MSNs, which, after calcination and drug loading, were then characterized using X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) technique, thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and diffuse reflectance ultraviolet-visible (DRS-UV-Vis) spectroscopy. Releases of DX from the MSNs were good in pH 7.4 (90%) phosphate buffer but poor in acidic pH (40%). In a comparative release study between the MSNs in phosphate buffer, TW60-3DX showed sustained release for 140 h, which was higher than the other nanoparticles. The mechanism of DX release from the MSNs was studied using Peppas kinetics model. The “n” value of all three MSNs ranged from 0.45 to 1 with a correlation coefficient (r2) >0.9, which indicated that the release of the drug from the system follows the anomalous transport or non-Fickian diffusion. The results supported the efficacy of mesoporous silica nanoparticles synthesized here as a promising carrier for duloxetine hydrochloride with higher drug loading and greater pH-sensitive release.
Electronic supplementary material
The online version of this article (doi:10.1208/s12249-014-0273-x) contains supplementary material, which is available to authorized users.KEY WORDS: controlled release, duloxetine hydrochloride, meso silica nanoparticles, sol–gel synthesis 相似文献16.
Onanong Nuchuchua Usawadee Sakulku Napaporn Uawongyart Satit Puttipipatkhachorn Apinan Soottitantawat Uracha Ruktanonchai 《AAPS PharmSciTech》2009,10(4):1234-1242
The nanoemulsions composed of citronella oil, hairy basil oil, and vetiver oil with mean droplet sizes ranging from 150 to
220 nm were prepared and investigated both in vitro and in vivo. Larger emulsion droplets (195–220 nm) shifted toward a smaller size (150–160 nm) after high-pressure homogenization and
resulted in higher release rate. We proposed that thin films obtained from the nanoemulsions with smaller droplet size would
have higher integrity, thus increasing the vaporization of essential oils and subsequently prolonging the mosquito repellant
activity. The release rates were fitted with Avrami’s equations and n values were in the same range of 0.6 to 1.0, implying that the release of encapsulated limonene was controlled by the diffusion
mechanism from the emulsion droplet. By using high-pressure homogenization together with optimum concentrations of 5% (w/w) hairy basil oil, 5% (w/w) vetiver oil (5%), and 10% (w/w) citronella oil could improve physical stability and prolong mosquito protection time to 4.7 h due to the combination of
these three essential oils as well as small droplet size of nanoemulsion. 相似文献
17.
In the present study, an attempt has been made to design controlled release colon-specific formulations of indomethacin by
employing pH responsive polymers Eudragit (L100 or S100) in matrix bases comprised of xanthan gum. The prepared tablets were
found to be of acceptable quality with low-weight variation and uniform drug content. In vitro release studies indicated rapid swelling and release of significant percentage of drug in the initial period from matrix
tablets composed of xanthan gum alone. Addition of pH responsive polymers Eudragit (L100 or S100) to xanthan gum matrix resulted
in negligible to very low drug release in the initial period in acidic to weakly acidic medium. Furthermore, with increase
in pH of the dissolution medium due to dissolution of Eudragit L100/Eudragit S100 that resulted in the formation of a porous
matrix, faster but controlled drug release pattern was observed. Thus, a sigmoidal release pattern was observed from the designed
formulations suitable for colonic delivery. Drug release mechanism in all cases was found to be of super case II type, indicating
erosion to be the primary cause of drug release. Since the drug release from almost all the matrix bases in the initial phase
was negligibly low and followed with controlled release for about 14–16 h, it was concluded that a matrix design of this composition
could have potential applications as a colon-specific drug delivery device with additional advantage of easy scale-up and
avoidance of all-or-none phenomenon associated with coated colon-specific systems. 相似文献
18.
The bioavailability of therapeutic agents from eye drops is usually limited due to corneal barrier functions and effective
eye protective mechanisms. Therefore, the current study aims to enhance ocular bioavailability of brimonidine, a potent antiglaucoma
drug, through the preparation of ocular inserts. Solvent casting technique was employed to prepare the inserts using polyvinylpyrrolidone
K-90 (PVP K-90) as film-forming polymer blended with different viscosity grades of bioadhesive polymers namely hydroxypropyl
methycellulose, carbopol, sodium alginate, and chitosan. The prepared ocular inserts were evaluated for various physicochemical
parameters, swelling behavior, and in vitro release patterns. Sodium alginate-based ocular inserts revealed the most sustainment in drug release (99% at 6 h), so it
was selected for further modifications via coating it, on one side or dual sides, using hydrophobic film composed of either
ethylcellulose or Eudragit RSPO. The obtained in vitro release results for the modified ocular inserts revealed that ethylcellulose is superior to Eudragit RSPO in terms of brimonidine
release sustainment effect. Ocular inserts composed of 7% PVP K-90, 1.5% low molecular weight sodium alginate with or without
ethylcellulose coat were able to sustain the in vitro release of brimonidine. Their therapeutic efficacy regarding intraocular pressure (IOP) lowering effect when inserted in
albino rabbits eyes showed superior sustainment effect compared with that of brimonidine solution. Furthermore, due to both
the mucoadhesive property and the drug sustainment effect, the one-side-coated ocular insert showed more IOP lowering effect
compared with that of its non-coated or dual-side-coated counterpart. 相似文献
19.
Nanomiemgel - A Novel Drug Delivery System for Topical Application - In Vitro and In Vivo Evaluation
Jaganmohan Somagoni Cedar H. A. Boakye Chandraiah Godugu Apurva R. Patel Henrique Antonio Mendonca Faria Valtencir Zucolotto Mandip Singh 《PloS one》2014,9(12)
AimThe objective of this study was to formulate and evaluate a unique matrix mixture (nanomiemgel) of nanomicelle and nanoemulsion containing aceclofenac and capsaicin using in vitro and in vivo analyses and to compare it to a marketed formulation (Aceproxyvon).MethodsNanomicelles were prepared using Vitamin E TPGS by solvent evaporation method and nanoemulsion was prepared by high-pressure homogenization method. In vitro drug release and human skin permeation studies were performed and analyzed using HPLC. The efficiency of nanomiemgel as a delivery system was investigated using an imiquimod-induced psoriatic like plaque model developed in C57BL/6 mice.ResultsAtomic Force Microscopy images of the samples exhibited a globular morphology with an average diameter of 200, 250 and 220 nm for NMI, NEM and NMG, respectively. Nanomiemgel demonstrated a controlled release drug pattern and induced 2.02 and 1.97-fold more permeation of aceclofenac and capsaicin, respectively than Aceproxyvon through dermatomed human skin. Nanomiemgel also showed 2.94 and 2.09-fold greater Cmax of aceclofenac and capsaicin, respectively than Aceproxyvon in skin microdialysis study in rats. The PASI score, ear thickness and spleen weight of the imiquimod-induced psoriatic-like plaque model were significantly (p<0.05) reduced in NMG treated mice compared to free drug, NEM, NMI & Aceproxyvon.ConclusionUsing a new combination of two different drug delivery systems (NEM+NMI), the absorption of the combined system (NMG) was found to be better than either of the individual drug delivery systems due to the utilization of the maximum possible paths of absorption available for that particular drug. 相似文献
20.
A gastro retentive floating drug delivery system with multiple-unit minitab’s based on gas formation technique was developed
in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists
of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of
an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates
(Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped
polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level
of gas-entrapped polymeric membrane decreased. The optimum system floated completely within 3 min and maintained the buoyancy
over a period of 12 h. The drug release was controlled and linear with the square root of time. Increasing coating level of
gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the controlled release properties
were achieved in the multiple-unit floating drug delivery system developed in this present study. The analysis of the parameter
dissolution data after storage at 40 °C and 75% RH for 3 months showed, no significant change indicating the two dissolution
profiles were considered to be similar (f2 value is more than 50). 相似文献