Dexibuprofen nanocrystals with improved therapeutic performance: fabrication, characterization, in silico modeling, and in vivo evaluation

Ullah, Naseem; Khan, Shahzeb; Ahmed, Shaimaa M.; Govender, Thirumala; Faidah, Hani; Matas, Marcel de; Shahid, Muhammad; Minhas, Muhammad Usman; Sohail, Muhammad; Khurram, Muhammad

doi:10.2147/ijn.s151597

Cited by 27 publications

(11 citation statements)

References 44 publications

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“…Consequently, a polymer combination that stabilizes the drug could be suggested. [39] 3.1.2 XRD analysis XRD analysis is an effective method for determining the exfoliation of fillers in the polymer matrix. Figure 1B shows the XRD pattern of GO, HPMC, and HPMC/5-FU@GO nanocomposite.…”

Section: Atr-ftir Analysismentioning

confidence: 99%

Hydroxypropyl methylcellulose/graphene oxide composite as drug carrier system for 5‐fluorouracil

Hasanin

El-Sakhawy

Ahmed

et al. 2022

Biotechnology Journal

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Aim: This study aims to prepare a nanocomposite (HPMC/5-FL@GO) from hydroxypropyl methylcellulose (HPMC) and graphene oxide (GO) as biocompatible materials.The nanocomposite enhances the drug activity of immobilized 5-fluorouracil (5-FU), decreasing the side effect of long-run treatment protocols with highly efficient drugdrug activity.Method and results: Different samples were characterized by ATR-FTIR spectroscopy, X-ray diffraction, scanning electron microscopy coupled with energy dispersive X-ray analysis, transmission electron microscopy, thermogravimetric analysis, and dynamic light scattering along with cytotoxicity and anticancer study. A homogenous and compatible nanocomposite structure with a homogenous drug distribution was confirmed.Furthermore, the prepared nanocomposite has a low cytotoxicity effect against normal Vero cell lines compared with 5-FU. The antitumor activities of the same nanocomposite (20.4 and 74.3 μg mL −1 on A549 and HepG-2) were lower than that of 5-FU (54.1 and 103 μg mL −1 on A549 and HepG-2). Conclusion and implications:According to the attained results, the HPMC/5-FL@GO can apply in a biomedical application such as cancer therapy with the unique biocompatible to human cells.

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Section: Atr-ftir Analysismentioning

confidence: 99%

Hydroxypropyl methylcellulose/graphene oxide composite as drug carrier system for 5‐fluorouracil

Hasanin

El-Sakhawy

Ahmed

et al. 2022

Biotechnology Journal

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“…Patterns observed for capsaicin and nanocrystals loaded with capsaicin were found to be quite similar, which may be due the non-homogenous mixing of the drug to the inactive moieties of formulation like Carbopol. Moreover, the peak at 2θ = 23 with capsaicin was disappeared due to the presence of Carbopol layer which encapsulated the drug effectively within the core of the nano-crystal formulation [27].…”

Section: Xrd Studiesmentioning

confidence: 99%

Fabrication of Capsaicin Loaded Nanocrystals: Physical Characterizations and In Vivo Evaluation

et al. 2021

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Nano-crystallization is a new emerging strategy to promote the saturation solubility, dissolution rate and subsequent bioavailability of Biopharmaceutical Class II drugs. Capsaicin belongs to BCS class-II drugs having low water solubility and dissolution rate. Nano-crystals (NC) of pure Capsaicin was developed and optimized in order to increase its water solubility, dissolution and further to promote its adhesiveness to skin epidermis layer. NC formulations were subjected to stability studies, droplet size, surface charge, poly-dispensability index, drug content, entrapment efficiency, thermal analysis, surface morphology, crystalline studies, solubility profile, in vitro release and ex vivo permeation studies. In vivo anti-inflammatory assay (Carrageenan-induced paw edema) was performed in Sprague Dawley rats. Nanocrystals loaded with capsaicin showed particle size 120 ± 3.0 nm with surface charge of −20.7 ± 3.5 and PDI was 0.48 ± 1.5. Drug content and entrapment efficiency of T3 was 85% and 90 ± 1.9% respectively. Thermal studies predicted that melting peak of capsaicin was present in the formulation suggested that there was no interaction between active moieties and excipients in NC formulation. Surface morphology confirmed the presence of Nano-size crystals having rough crystalline surface. XRD proved that the capsaicin NC are successfully developed by using high speed homogenization. The solubility of capsaicin was found to be 12.0 ± 0.013 μg/mL in water. In vitro study revealed that 89.94 ± 1.9% of drug was released within 24 h. Similarly, drug permeation was 68.32 ± 1.83%, drug retained in skin was 16.13 ± 1.11% while drug retained on skin was 9.12 ± 0.14% after 12 h. The nanocrystals showed higher anti-inflammatory activity as compared to marketed product (Dicloran®). The study concluded that improvement in dissolution rate of capsaicin may potentially provide the opportunities in the development of a much cost-effective dosage forms that will produce improved pharmacological effects, but at low dose as compared to the already available products.

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“…As aforementioned, PU-NCs were fabricated using an antisolvent precipitation approach. , Briefly, 0.25 mL of acetone containing PU (20 mg/mL) was quickly injected into 10 mL of H 2 O containing hydroxypropyl methylcellulose E3 (HPMC E3, 1 mg/mL), followed by 1000 r/min stirring at room temperature. Meanwhile, a single factor design was performed to optimize the PU-NCs formulation, by varying stabilizer types and concentrations, PU concentrations, and antisolvent-to-solvent ratios.…”

Section: Materials and Methodsmentioning

confidence: 99%

Oral Delivery of Puerarin Nanocrystals To Improve Brain Accumulation and Anti-Parkinsonian Efficacy

Xiong

Liu

et al. 2019

Mol. Pharmaceutics

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Puerarin (PU) has emerged as a promising herbderived anti-Parkinsonism compound. However, the undesirable water solubility as well as the unwanted bioavailability of PU limit its application. Therefore, this study aimed to develop and characterize PU nanocrystals (PU-NCs) with enhanced oral bioavailability and improved brain accumulation for the treatment of Parkinson's disease (PD). The fabricated PU-NCs were approximately spherical, with a mean size of 83.05 ± 1.96 nm, a PDI of 0.047 ± 0.009, a drug loading of 72.7%, and a rapid dissolution rate in vitro. Molecular dynamics simulation of PU and Pluronic F68 demonstrated the interaction energy and binding energy of −88.1 kJ/mol and −40.201 ± 0.685 kJ/mol, respectively, indicating a spontaneous binding with van der Waals interactions. In addition, the cellular uptake and permeability of PU-NCs were significantly enhanced as compared to PU alone (p < 0.01). Moreover, PU-NCs exerted a significant neuroprotective effect against the cellular damage induced by the 1-methyl-4phenylpyridinium ion (MPP + ). Besides, PU-NCs demonstrated no obvious toxic effects on zebrafish, as evidenced by the unaltered morphology, hatching, survival rate, body length, and heart rate. Fluorescence resonance energy transfer (FRET) imaging revealed that intact nanocrystals were found in the intestine and brain of adult zebrafish gavaged with DiO/DiI/PU-NCs. Increased values of C max and AUC 0−t were observed in the plasma of rats following oral administration of PU-NCs compared to PU suspension. Likewise, brain accumulation of PU-NCs was higher than that of PU suspension. Furthermore, PU-NCs attenuated dopamine depletion, ameliorated 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced behavioral deficits, and enhanced the levels of dopamine and its metabolites. Taken altogether, this study provides evidence that PU-NCs could be exploited as a potential oral delivery system to treat PD, by improving the poor bioavailability of PU and enhancing their delivery into the brain.

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Dexibuprofen nanocrystals with improved therapeutic performance: fabrication, characterization, in silico modeling, and in vivo evaluation

Cited by 27 publications

References 44 publications

Hydroxypropyl methylcellulose/graphene oxide composite as drug carrier system for 5‐fluorouracil

Hydroxypropyl methylcellulose/graphene oxide composite as drug carrier system for 5‐fluorouracil

Fabrication of Capsaicin Loaded Nanocrystals: Physical Characterizations and In Vivo Evaluation

Oral Delivery of Puerarin Nanocrystals To Improve Brain Accumulation and Anti-Parkinsonian Efficacy

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