Novel nanosized formulations of two diclofenac acid polymorphs to improve topical bioavailability

Pireddu, Rosa; Sinico, Chiara; Ennas, Guido; Marongiu, Francesca; Muzzalupo, Rita; Lai, Francesco; Fadda, Anna Maria

doi:10.1016/j.ejps.2015.06.006

Cited by 62 publications

(32 citation statements)

References 25 publications

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“…All those analytical data demonstrate that the size reduction during the nanosuspension formulation process did not influence the RSV crystalline pattern and, furthermore, in the FTIR spectrum, the stretching at 965 cm −1 confirmed that the process did not afford the isomerization of the RSV trans double bond [15]. Raw and nanosized RSV particle features were analyzed and compared by means of SEM images, as shown in ▶ Fig.…”

Section: Resultsmentioning

confidence: 88%

Enhancing Topical Delivery of Resveratrol through a Nanosizing Approach

et al. 2016

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Resveratrol is a naturally occurring polyphenol with strong antioxidant and free radical scavenging properties, recently proposed as a therapeutic agent for skin diseases. In this study, we investigated the possibility of improving the dermal bioavailability of the poorly water-soluble drug resveratrol by nanocrystal technology. To this purpose, nanosuspensions were prepared by the wet media milling technique, using Poloxamer 188 or Tween 80 as stabilizers, and characterized by means of both solid state and morphological and dimensional studies. All analytical data demonstrated that neither a modification of the drug crystalline pattern nor the isomerization of the double bond were observed after the wet media milling particle size reduction process, which produced rounded and smooth nanocrystals with a mean diameter ranging between 0.2-0.3 µm. Resveratrol skin delivery from nanosuspension formulations was evaluated by the pig ear skin model via tape stripping. Results of the experiments showed that after application of nanosuspension formulations, higher amounts of resveratrol could penetrate the skin at deeper levels compared to drug coarse suspensions. The antioxidant activity of resveratrol in nanocrystals was assessed by the DPPH assay, which demonstrated that the size reduction process as well as the formulation compositions did not modify the drug antioxidant activity.

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Section: Resultsmentioning

confidence: 88%

Enhancing Topical Delivery of Resveratrol through a Nanosizing Approach

et al. 2016

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“…In this case, the solubility was increased not only due to the smaller particle size, but also due to the formation of the higher energy solid-state forms. Pireddu et al studied two different diclofenac sodium crystal forms for transdermal drug delivery [ 29 ]. Nanocrystals were produced by wet ball milling, with poloxamer 188 used as a stabilizer.…”

Section: Characterization Of Nanocrystalsmentioning

confidence: 99%

Performance Parameters and Characterizations of Nanocrystals: A Brief Review

2016

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Poor bioavailability of drugs associated with their poor solubility limits the clinical effectiveness of almost 40% of the newly discovered drug moieties. Low solubility, coupled with a high log p value, high melting point and high dose necessitates exploration of alternative formulation strategies for such drugs. One such novel approach is formulation of the drugs as “Nanocrystals”. Nanocrystals are primarily comprised of drug and surfactants/stabilizers and are manufactured by “top-down” or “bottom-up” methods. Nanocrystals aid the clinical efficacy of drugs by various means such as enhancement of bioavailability, lowering of dose requirement, and facilitating sustained release of the drug. This effect is dependent on the various characteristics of nanocrystals (particle size, saturation solubility, dissolution velocity), which have an impact on the improved performance of the nanocrystals. Various sophisticated techniques have been developed to evaluate these characteristics. This article describes in detail the various characterization techniques along with a brief review of the significance of the various parameters on the performance of nanocrystals.

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“…24 More recently, alginatechitosan loaded drugs have been developed to improve the bioavailability of a large number of drugs. [19][20][21][22][23][24]26,27 Mean Particle Size, Poly Disparity Index, and Zeta Potential…”

Section: Results and Discussion Formulation Development And Optimizationmentioning

confidence: 99%

“…18 Other research studies have described the oral delivery of microspheres, consisting of Alginate (ALG) and Chitosan (CS) as mucoadhesive polymers. These microspheres were successfully combined with various drugs, such as glipizide, 19 insulin, 20 ranitidine, 21 metformin, 22 diclofenac, 23 and various other drugs, 24 and showed improved solubility and bioavailability.…”

Section: Introductionmentioning

confidence: 99%

<p>The Oral Administration of Lidocaine HCl Biodegradable Microspheres: Formulation and Optimization</p>

AlQuadeib

Eltahir

Alagili

2020

IJN

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Purpose: Lidocaine (LID) is a local anesthetic that is administered either by injection and/or a topical/transdermal route. However, there is a current need to develop efficacious methods for the oral delivery of LID with optimized bioavailability. Methods: We developed oral LID biodegradable microspheres that were loaded with alginate-chitosan with different mass ratios, and characterized these microspheres in vitro. We also developed, and utilized, a simple and sensitive HPLC-tandem mass spectrometry (LC-MS-MS) method for assaying LID microspheres. Results: The mean particle size (MPS) of the LID microspheres ranged from 340.7 to 528.3 nm. As the concentration of alginate was reduced, there was a significant reduction in MPS. However, there was no significant change in drug entrapment efficiency (DEE), or drug yield, when the alginate concentration was either increased or decreased. DSC measurements demonstrated the successful loading of LID to the new formulations. After a slow initial release, less than 10% of the LID was released in vitro within 4 h at pH 1.2. In order to evaluate nephrotoxicity, we carried out MTT assays of LID in two types of cell line (LLC-PK1 and MDCK). LID significantly suppressed the cell toxicity of both cell lines at the concentrations tested (100, 200, and 400ng/µL). Conclusion: Experiments involving the oral delivery of LID formulations showed a significant reduction in particle size and an improvement in dissolution rate. The formulations of LID developed exhibit significantly less toxicity than LID alone.

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Novel nanosized formulations of two diclofenac acid polymorphs to improve topical bioavailability

Cited by 62 publications

References 25 publications

Enhancing Topical Delivery of Resveratrol through a Nanosizing Approach

Enhancing Topical Delivery of Resveratrol through a Nanosizing Approach

Performance Parameters and Characterizations of Nanocrystals: A Brief Review

<p>The Oral Administration of Lidocaine HCl Biodegradable Microspheres: Formulation and Optimization</p>

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