Combination of synthetic and natural polymers in hydrogel: An impact on drug permeation (original) (raw)
Related papers
Current Drug Delivery, 2009
In this study the effect of vehicle on in vitro diffusion of diclofenac sodium (DS) from new different formulations such as Carbopol gel (A), Sodium lauryl sulphate cream (B) and Carbopol cream (C) was evaluated with Franz diffusion cells using hydrophilic and hydrophobic synthetic membranes. The commercial formulation Voltaren ® Emulgel was used as reference. Furthermore, the in vivo efficacy of topical formulations was studied in the carrageenan-induced edema and hyperalgesia, whereas the antinociceptive effect was evaluated on thermal pain threshold in rat paw. The flux of DS across hydrophilic membranes showed this rank order: Control C > A B. On the other hand, the diffusion rate of DS across hydrophobic membranes resulted in the following order: Control > B > A C; this suggested a lower interaction between the vehicles and these membranes. The in vivo results indicated that the prepared formulations failed in the inflammatory tests to reduce the development of edema. Nevertheless, treatment with B formulation inhibited the development of acute hyperalgesia induced by carrageenan, and elicited a significant increase in paw withdrawal latencies whereas other formulations were ineffective. The results obtained in this study suggest that Sodium lauryl sulphate cream might be useful in local pain conditions and may be an effective alternative to the presently used systemic routes.
International Journal of PharmTech …, 2010
The comparative in vitro skin permeability of diclofenac sodium through excised mouse skin from different common pharmaceutical vehicles like castor oil, olive oil, arachis oil, liquid paraffin, white soft paraffin melt, 3% sodium carboxymethyl cellulose (CMC) aqueous gel and isopropyl myristate (IPM), excluding other excipients was evaluated. Significantly (p < 0.05) higher flux of diclofenac sodium (0.26 ± 0.01 mg/cm 2 /hr) was provided by isopropyl myristate as vehicle than other vehicles used. Maximum permeability coefficient and diffusion coefficient were also observed for isopropyl myristate and minimum in case of white soft paraffin melt. But, isopropyl myristate had minimal lag time (0.60 ± 0.05 hr); while, maximum lag time (0.86 ± 0.05 hr) was observed for white soft paraffin melt. We have also investigated the in-vitro skin permeability of diclofenac sodium through excised mouse skin from liquid paraffin and olive oil with addition of 0.1 % menthol and dried Aloe vera juice as permeation enhancers. Flux, permeability coefficient, diffusion coefficient and enhancement ratio were better in the case of liquid paraffin with 0.1 % menthol as permeation enhancer than others. We believe this investigation is considered to be useful in preformulation step to predict the best vehicle in further experiment and also provides valuable data that can be utilized for designing and development of various topical formulations of diclofenac sodium.
Comparison of skin permeability for three diclofenac topical formulations: an in vitro study
Die Pharmazie, 2014
Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug (NSAID) widely used in humans and animals. There are limited published studies evaluating diclofenac's skin permeation following topical administration. The aim of our study was to evaluate and compare the in vitro permeation of three different diclofenac-containing formulations (patch, gel, solution) over 24 hours. These formulations were applied (n = 6 per formulation) to pig skin sandwiched between the two chambers in a static Franz diffusion cell and aliquots from the receptor medium were sampled at pre-defined time points. An HPLC method with UV detection was developed and validated with the aim of characterizing the transepidermal penetration in the in vitro system. Using this assay to determine the permeation parameters, results at 24 hours showed that the Flector patch released the highest drug amount (54.6%), whereas a lower drug amount was delivered with the Voltaren Emulgel (38.2%) and the solution (34.4...
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...
Effect of rubbing on the in vitro skin permeation of diclofenac-diethylamine 1.16% gel
BMC Research Notes, 2012
Background: Rubbing a topical NSAID (non steroidal anti-inflammatory drug) on the skin may increase local drug permeation, affecting its distribution to the site of pain and inflammation. The present study evaluates this hypothesis, by assessing in vitro the effect on skin permeation of applying diclofenac-dieythylamine 1.16% gel with or without rubbing. Methods: A single dose of 5 mg/cm 2 diclofenac-diethylamine 1.16% gel was applied on excised human skin mounted in Franz-type diffusion cells without or with rubbing for 45 s. Drug penetration into the skin layers was determined after 1 h using the tape stripping technique. In vitro cutaneous permeation into the receptor fluid of the diffusion chamber was measured up to 24 h. Skin electrical resistance was also recorded. Results: Application of diclofenac-diethylamine 1.16% gel with rubbing resulted to a 5-fold higher flux of diclofenac through the skin than when applied without rubbing at 8 h (P = 0.04). Skin rubbing for 45 s decreased by 2-fold skin electrical resistance when compared to the standard application. Application of diclofenac-diethylamine 1.16% gel with rubbing tended to result in higher accumulation in the stripped skin vs. the superficial skin layers when applied without rubbing (P = 0.2). Conclusion: These results suggest that rubbing may alter the superficial skin layer resulting in a transient faster initial diffusion of topically applied diclofenac through the stratum corneum into the deeper skin layer of the dermis to the tissue target.
A Research Article on Nanogel as Topical Promising Drug Delivery for Diclofenac sodium
Indian Journal of Pharmaceutical Education and Research, 2017
Background: Transdermal delivery of drug is promising but challenging system is available for local as well as systemic effect of drug. The prolonged residence of drug formulation in the skin is important for transdermal drug delivery. Objective: The objective of the present investigation was to develop a nanogel with reduced particle size in order to improve the bioavailability of the anti-inflammatory drug, Diclofenac sodium. Methods: The present study is to formulate nanosizes dispersion of diclofenac sodium by emulsionsolvent diffusion method and incorporation of gelling agent to produce nanogel. The formulation are characterized for particle size ranging from 100-400 nm. A drug named diclofenac sodium used in rheumatoid disorders and chronic inflammatory diseases. Results: Glycerol: Water (20:80) co-solvent system is selected for preparing diclofenac sodium nanogels using different polymers and has better permeability coefficient than alcohol: water co-solvent. Permeation through cellophane membrane was carried using 0.9% w/v sodium chloride using receptor fluid in franz diffusion cell (1.74 cm 2). Gels containing diclofenac sodium with eudragit polymer shown better permeability coefficient. Conclusion: Diclofenac sodium nanogels formulated using carbopol with permeation enhancer has shown better flux enhancement in comparison with nanogels formulated using HPMC and methyl cellulose. It has been concluded that diclofenac sodium nanogels using carbopol 940 as gelling agent and Eudragit S-100 has shown better flux enhancement with propylene glycol as permeation enhancer.
FORMULATION AND IN -VITR0 EVALUATION OF NSAID's GEL
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), Polyethylene glycol exhibited little or no effect on the permeation characteristics of diclofenac sodium. The samples withdrawn were spectrophotometrically estimated at 256nm against their respective blank. These types of topical dosage forms could give sustained delivery of drug onto the skin, so they are interesting promises to improve skin absorption of nonsteroidal anti-inflammatory drugs and to prevent side effects associated. The gel preparation is excellent in the percutaneous absorption of diclofenac or its salts and provides good properties upon use and superior medical effects of diclofenac or its salts.
Transdermal delivery of diclofenac sodium through rat skin from various formulations
AAPS PharmSciTech, 2006
The aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of w/o microemulsion (M) and gel (G) bases for diclofenac sodium (DS). The effect of dimethyl sulfoxide (DMSO) as a penetration enhancer was also examined when it was added to the M formulation. To study the in vitro potential of these formulations, permeation studies were performed with Franz diffusion cells using excised dorsal rat skin. To investigate their in vivo performance, a carrageenan-induced rat paw edema model was used. The commercial formulation of DS (C) was used as a reference formulation. The results of the in vitro permeation studies and the paw edema tests were analyzed by repeated-measures analysis of variance. The in vitro permeation studies found that M was superior to G and C and that adding DMSO to M increased the permeation rate. The permeability coefficients (Kp) of DS from M and M+DMSO were higher (Kp = 4.9 × 10 −3 ± 3.6 × 10 −4 cm/h and 5.3 × 10 −3 ± 1.2 × 10 −3 cm/h, respectively) than the Kp of DS from C (Kp = 2.7 × 10 −3 ± 7.3 × 10 −4 cm/h) and G (Kp = 4.5 × 10 −3 ± 4.5 × 10 −5 cm/h). In the paw edema test, M showed the best permeation and effectiveness, and M+DMSO had nearly the same effect as M. The in vitro and in vivo studies showed that M could be a new, alternative dosage form for effective therapy.
Surfactant effects on the in vitro percutaneous absorption of diclofenac sodium
European Journal of Drug Metabolism and Pharmacokinetics, 1998
Nonionic surfactants, which are a safe class of enhancers, may offer means of enhancing drug permeation through the skin. In order to determine this effect, the influence of four nonionic surfactants on the percutaneous absorption of diclofenac sodium from carbopol gels containing 40% propylene glycol was investigated. In vitro diffusion experiments were carried out using excised full-thickness abdominal rat skin as well as cellulose nitrate membranes. The data of this study clearly revealed that Tween 80 decreased diclofenac penetration rate. This was due to a decrease in thermodynamic activity as a result of micellar complexation. In contrast, the more hydrophobic sorbitans enhanced diclofenac skin penetration, probably due to changes in the barrier properties of the skin and in the vehicle-stratum corneum partition coefficient. The most enhancing effect was induced by Span 20, a surfactant with a C12 saturated hydrophobic group. However, diffusional lag times for all the tested surfactants were longer than for the control gel.
Formulation and in vitro evaluation of transdermal matrix patches of Diclofenac sodium
2011
In this work an attempt was made to formulate and evaluate transdermal matrix patches for controlled delivery of diclofenac sodium. Low molecular weight, shorter half-life and low oral bioavailability due to first pass metabolism of diclofenac sodium made it a suitable drug candidate for the development of transdermal patches. Matrix-type transdermal patches containing diclofenac sodium were prepared using different ratios of ethylcellulose (EC) and polyvinylpyrrolidone K-30 (PVP K-30) by solvent evaporation technique. All the patches were evaluated for the permeation along with physicochemical studies including thickness, weight variation, moisture content, moisture uptake, flatness, folding endurance and drug content. The results of physical parameters ensured integrity and applicability of the patches. The in vitro drug permeation was best fitted with the zero order kinetics. Also the diffusion coefficient of release profiles (slope) had a value of > 1, which indicated super case II transport. Based on the above observations, it can be reasonably concluded that the release pattern of diclofenac sodium can be controlled by maintaining appropriate proportion of EC and PVP-K30 in the matrix patch.