This study was aimed to develop a simple and reproducible spectrophotometric method for the characterization of diclofenac sodium (DS) and to evaluate the efficacy of orally administered liposome encapsulated as well as free form DS in animal model. A simple, rapid and economical spectrophotometric analytical procedure with estimation in UV-visible region was performed on DS using dimethyl sulfoxide as solvent. Parameters such as time, temperature and types of solvent were studied for 20 μg/mL DS solution at 295 nm. All parameters and results of analysis were statistically validated. Liposome-encapsulated and free form DS samples were subjected to characterization study that includes entrapment efficacy determination and particle size analysis. Drug samples were further tested for their in vivo anti-inflammatory efficacy using histamine-induced paw edema test. Under optimized parameters, the Beer's law is obeyed in range of 0.625-40 μg/mL at λmax 295 nm. A linear working range of 5-35 μg/mL with regression coefficient of 0.9978 was obtained by using seven triplicate analyses of drug samples at seven different concentrations. The limit of detection and limit of quantitation was 1.19 and 3.62 μg/mL, respectively. Result of characterization study showed that the optimum formulation, which has high entrapment efficacy of 87 %, homogenous in size (polydispersity index 0.27), stable and reproducible, were obtained by using the Pro-Lipo Duo with 10 h hydration time and 16 mg/g DS. The liposome encapsulated DS resulted in significant (P < 0.05) inhibition up to 86 % in histamine-induced paw edema test. Present study successfully demonstrated an optimized procedure as per ICH guidelines in detection and evaluation of DS. In addition, nanoencapsulation of DS using liposome was found to demonstrate a potential enhancement in therapeutic efficacy.
Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, antinociceptive, and antipyretic activities. Liposomes have been shown to improve the therapeutic efficacy of encapsulated drugs. The present study was conducted to compare the antinociceptive properties between liposome-encapsulated and free-form diclofenac in vivo via different nociceptive assay models. Liposome-encapsulated diclofenac was prepared using the commercialized proliposome method. Antinociceptive effects of liposome-encapsulated and free-form diclofenac were evaluated using formalin test, acetic acid-induced abdominal writhing test, Randall–Selitto paw pressure test, and plantar test. The results of the writhing test showed a significant reduction of abdominal constriction in all treatment groups in a dose-dependent manner. The 20 mg/kg liposome-encapsulated diclofenac demonstrated the highest antinociceptive effect at 78.97% compared with 55.89% in the free-form group at equivalent dosage. Both liposome-encapsulated and free-form diclofenac produced significant results in the late phase of formalin assay at a dose of 20 mg/kg, with antinociception percentages of 78.84% and 60.71%, respectively. Significant results of antinociception were also observed in both hyperalgesia assays. For Randall–Sellito assay, the highest antinociception effect of 71.38% was achieved with 20 mg/kg liposome-encapsulated diclofenac, while the lowest antinociceptive effect of 17.32% was recorded with 0 mg/kg liposome formulation, whereas in the plantar test, the highest antinociceptive effect was achieved at 56.7% with 20 mg/kg liposome-encapsulated diclofenac, and the lowest effect was shown with 0 mg/kg liposome formulation of 8.89%. The present study suggests that liposome-encapsulated diclofenac exhibits higher antinociceptive efficacy in a dose-dependent manner in comparison with free-form diclofenac.
This study was conducted to compare the anti-inflammatory efficacy of nanoencapsulated and freeform diclofenac in rat. Diclofenac-Ioaded Iiposomes were prepared using the proliposome method. The anti-inflammatory effects ofnanoencapsulated and free diclofenac were evaluated using the carrageenaninduced paw edema, formalin-induced paw licking and cotton-pellet-induced granuloma tests in vivo. For carrageenan-induced paw edema, 2 and 20 mg/kg Iiposome-encapsulated diclofenac showed significant paw volume reduction compared to free form diclofenac of equivalent dosage groups. In the formalin test, significant reduction in paw-licking time was observed in late phase for both Iiposomeencapsulated and free-form diclofenac (2 and 20 mg/kg) with the percentage of inhibition of 28.62, 60.17% for free-form diclofenac and 31.45, 78.84% for Iiposome-encapsulated diclofenac, respectively. In cotton-pellet-induced granuloma test 20 mg/kg free-form diclofenac showed significant reduction in the size of granuloma in both transudative and granuloma weight with percentage of inhibition of 42.93 and 49.26%, respectively, when compared to controls. Interestingly, 20 mg/kg nanoencapsulated diclofenac showed a larger reduction of the parameter with percentage of inhibition of 48.43 and 63.55%, respectively. Collectively, these results indicated that nanoencapsulated diclofenac exhibited statistically higher efficacy than free-form diclofenac when orally administered. Hence, clinical dosage may be reduced thereby reducing the drug's adverse effects.
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