Investigations on Analgesic, Anti-inflammatory and Ulcerogenic Potential of Meloxicam Solid Dispersion Prepared with Skimmed Milk

Mishra, Dina Nath; Kumar, Sengodan Gurusamy Vijaya

doi:10.1248/yakushi.126.495

Cited by 5 publications

(5 citation statements)

References 14 publications

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“…Stomachs were placed on a corkboard and pinned, the ulcer score was done by examining under the dissection microscope. A blind observer unaware of the experimental groups was requested to assess the mucosal damage.Scoring sheet (Mishra and Vijay Kumar, 2006) containing the following rubrics was used for scoring 0-no injury or bleeding 1-slight injury (two to three dots) 2-severe injury (hemorrhagic streaks, five to six dots) 3-very severe injury (many lined injuries) 4-mucosa full of lesions…”

Section: Ulcerogenic Studymentioning

confidence: 99%

“…The gastric retention of oral solutions containing these drugs could be favorably achieved through a radical approach of the liquid insitu gelling system. These systems are polymeric gel formulations that respond to physical or chemical signals, including pH, ionic factor, metabolite, or temperature (Kubo et al, 2003;Miyazaki et al, 2001;Prabaharan and Mano, 2006). Numerous polymers such as pectin (Ghare and Mundada, 2017), chitosan (Belhadji et al, 2017), gellan gum (Kerdsakundee et al, 2016), xyloglucan, and xanthan gum have been investigated for this purpose.…”

Section: Introductionmentioning

confidence: 99%

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Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam

2018

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The present study was aimed to develop gastric floating in-situ gels of meloxicam (MLX) mainly to enhance antiinflammatory activity and alleviate gastric ulceration potential of meloxicam. Ternary inclusion complex of meloxicam containing hydrox ypropyl beta cyclodextrin (HPβCD) and diethylamine (DEA) in 1:1:1 molar ratio was used as a chief component in the development of gastric floating in-situ gel formulations of meloxicam. Box-Behnken design was utilized to design and optimize gastric floating in-situ gels of meloxicam. Independent variables (concentrations of sodium alginate, calcium carbonate, and a ternary inclusion complex of meloxicam, respectively) were optimized in order to achieve the desired responses. The response surface plots and the possible interactions between the independent variables were analyzed using the Design Expert Software 11.0.3.0 (Stat-Ease, Inc, USA). The results showed that the optimized gastric floating in-situ gels with a short floating lag time (41 seconds), low viscosity (190 cps), and high in vitro drug release at sixth hour (77%) was obtained using an optimized combination of calcium carbonate (0.75% w/v), sodium alginate (1.25% w/v), and MLX-HPβCD-DEA ternary complex (equivalent to 11.25 mg of meloxicam), respectively. Moreover, the optimized gastric floating in-situ gel formulation of meloxicam ternary complex exhibited significantly ameliorated anti-inflammatory activity [84.38% (p < 0.05) at sixth hour and also showed a significant reduction in local gastric ulceration potential compared to pure meloxicam]. Thus, this gastric floating in situ gelling system can be translated for existing and established non-steroidal anti-inflammatory drugs (NSAID) as well as formulations.

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Section: Ulcerogenic Studymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam

2018

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“…Solid dispersions of Meloxicam were prepared with skimmed milk using rotary vacuum evaporation technique with enhanced aqueous solubility and dissolution rate due to presence of lactose in skimmed which provide polar effect and also due to reduced crystallinity of the drug (36).…”

Section: Miscellaneousmentioning

confidence: 99%

Natural polymers: Best carriers for improving bioavailability of poorly water

Sapkal¹,

Narkhede²,

Babhulkar³

et al. 2013

mpj

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Solid dispersion techniques have been used to enhance the dissolution and oral bioavailability of many poorly water soluble drugs (1). To overcome the solubility problem discussed above, many authors formulated solid dispersions using number of various polymers and methods. In spite of tremendous research activity on solid dispersions since 1961, their commercial application is limited. Only a few products have been marketed so far. One aspect of solid dispersion technology on which most workers in the field would agree is that the number of marketed products arising from this approach has been disappointing. Research for alternative carriers has been increasing to suit for the industrial applications as well as to reduce the production cost and toxic effects. Recently, many natural polymers have been evaluated for their uses in formulation of solid disper-ABSTRACT Natural polymers and its modified forms can be used as best alternative for improving bioavailability of poorly water soluble drugs in solid dispersion. Most of the natural polymers are hydrophilic and having high swelling capacity. Recent trend towards the use of natural polymer demands the replacement of synthetic additives with natural ones. Many plant derived natural polymers are studied for use in solid dispersion systems, out of which natural gums, cyclodextrin and carbohydrate are most extensively studied and used. This review discusses about the majority of these natural polymers, its uses and some recent investigations about modification of natural polymer in solid dispersion systems.

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“…NSAIDs are reported to remain in crystalline form in the acidic medium of the stomach. 4,5 This crystalline form can be accounted for the prolonged contact of these drugs with the gastric mucosa with consequent high local concentration and irritation-induced ulceration.…”

Section: Introductionmentioning

confidence: 99%

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

El-Habashy

Allam

El-Kamel

2016

IJN

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Nanoparticles (NPs) have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong drug release, and decrease side effects of highly toxic drugs. The objective of this investigation was to evaluate the potential of ethyl cellulose-based NPs (EC-NPs) to modulate the release and reduce ulcerogenicity of piroxicam (PX) after oral administration. PX-loaded EC-NPs were prepared by solvent evaporation technique using different stabilizers at three concentration levels. Morphological examination of selected formulas confirmed the formation of spherical NPs with slightly porous surface. Formulation containing poloxamer-stabilized EC-NPs (P188/0.2), having a particle size of 240.26±29.24 nm, polydispersity index of 0.562±0.030, entrapment efficiency of 85.29%±1.57%, and modulated release of PX (88% after 12 hours), was selected as the optimum formulation. Differential scanning calorimetry demonstrated the presence of PX in an amorphous form in the NPs. Fourier-transform infrared spectroscopy revealed the possible formation of hydrogen bond and the absence of chemical interaction. In vivo study, evaluation of pharmacokinetic parameters, evaluation of gastric irritation potential, and histological examination were conducted after administration of the selected formulation. Time to reach maximum plasma concentration, t max , of poloxamer-stabilized EC-NPs was significantly higher than that of Feldene ® 20 mg capsules ( P ≤0.001). Encapsulation of the acidic, gastric offender PX into NPs managed to significantly suppress gastric ulceration potential in rats ( P ≤0.05) as compared to that of PX suspension. A reduction of 66% in mean ulcer index was observed. In conclusion, poloxamer-stabilized EC-NPs (P188/0.2) had a significant potential of offsetting deleterious side effects common in PX use.

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Investigations on Analgesic, Anti-inflammatory and Ulcerogenic Potential of Meloxicam Solid Dispersion Prepared with Skimmed Milk

Cited by 5 publications

References 14 publications

Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam

Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam

Natural polymers: Best carriers for improving bioavailability of poorly water

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

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