Ricobendazole nanocrystals obtained by media milling and spray drying: Pharmacokinetic comparison with the micronized form of the drug

Paredes, Alejandro J.; Camacho, Nahuel Matías; Schofs, Laureano; Dib, Alicia; Zarazaga, María del Pilar; Litterio, Nicolás Javier; Allemandi, Daniel Alberto; Bruni, Sergio Fabian Sanchez; Lanusse, Carlos; Palma, Santiago Daniel

doi:10.1016/j.ijpharm.2020.119501

Cited by 55 publications

(28 citation statements)

References 39 publications

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“…These results are indicating that there are some crystallinity changes and potential interactions may have occurred between the drug and the polymer. Finally, the implants showed a broader melting peak for OLZ, and they have shifted toward lower temperatures, which could be attributed to a thermally induced amorphization of the blend during DSC experiment (Paredes et al., 2020 ).…”

Section: Resultsmentioning

confidence: 99%

3D-printed implantable devices with biodegradable rate-controlling membrane for sustained delivery of hydrophobic drugs

et al. 2022

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Implantable drug delivery systems offer an alternative for the treatments of long-term conditions (i.e. schizophrenia, HIV, or Parkinson’s disease among many others). The objective of the present work was to formulate implantable devices loaded with the model hydrophobic drug olanzapine (OLZ) using robocasting 3D-printing combined with a pre-formed rate controlling membrane. OLZ was selected as a model molecule due to its hydrophobic nature and because is a good example of a molecule used to treat a chronic condition schizophrenia. The resulting implants consisted of a poly(ethylene oxide) (PEO) implant coated with a poly(caprolactone) (PCL)-based membrane. The implants were loaded with 50 and 80% (w/w) of OLZ. They were prepared using an extrusion-based 3D-printer from aqueous pastes containing 36–38% (w/w) of water. The printing process was carried out at room temperature. The resulting implants were characterized by using infrared spectroscopy, scanning electron microscopy, thermal analysis, and X-ray diffraction. Crystals of OLZ were present in the implant after the printing process. In vitro release studies showed that implants containing 50% and 80% (w/w) of OLZ were capable of providing drug release for up to 190 days. On the other hand, implants containing 80% (w/w) of OLZ presented a slower release kinetics. After 190 days, total drug release was ca. 77% and ca. 64% for implants containing 50% and 80% (w/w) of OLZ, respectively. The higher PEO content within implants containing 50% (w/w) of OLZ allows a faster release as this polymer acts as a co-solvent of the drug.

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Section: Resultsmentioning

confidence: 99%

3D-printed implantable devices with biodegradable rate-controlling membrane for sustained delivery of hydrophobic drugs

et al. 2022

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“…This method forms NCs according to mechanical abrasion to transform large crystalline particles into nanosized particles. 53 Compared to the bottom up technique, this method has been reported to be more likely to maintain the crystalline form of the particles. 54 Several stabilizers were screened, including Tween 80, PVA, and P127, with different concentrations.…”

Section: Resultsmentioning

confidence: 99%

“…Specifically, the top down technique using modified media milling was selected. This method forms NCs according to mechanical abrasion to transform large crystalline particles into nanosized particles . Compared to the bottom up technique, this method has been reported to be more likely to maintain the crystalline form of the particles .…”

Section: Resultsmentioning

confidence: 99%

Albendazole Nanocrystal-Based Dissolving Microneedles with Improved Pharmacokinetic Performance for Enhanced Treatment of Cystic Echinococcosis

Permana

Paredes

Volpe‐Zanutto

et al. 2021

ACS Appl. Mater. Interfaces

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Cystic echinococcosis (CE) is a zoonosis caused by Echinococcus spp., affecting both humans and animals’ lives. Current treatment of CE by oral administration of albendazole (ABZ) is hampered by several limitations. The poor aqueous solubility and the rapid metabolism of ABZ in the liver are the main issues, leading to lack of efficacy of the treatment. In the present study, we developed a nanocrystalline (NC) formulation of ABZ to be delivered intradermally using dissolving microneedles (DMNs). The NC formulation was developed using milling in an ultrasmall-scale device. Following several screenings, Pluronic F127 was selected as a suitable stabilizer, producing NCs with around 400 nm in size with narrow particle distribution. The crystallinity of ABZ was maintained as observed by DSC and XRD analysis. The NC approach was able to improve the dissolution percentage of ABZ by approximately three-fold. Furthermore, the incorporation of NCs into DMNs using the combination of poly(vinylpyrrolidone) and poly(vinyl alcohol) formed sharp needles with sufficient mechanical strength and insertion properties. Dermatokinetic studies revealed that >25% of ABZ was localized in the dermis of excised neonatal porcine skin up to 48 h after DMN administration. In in vivo pharmacokinetic studies, the AUC and relative bioavailability values of ABZ delivered by NC-loaded DMNs were found to be significantly higher than those obtained after oral administration of coarse suspension of ABZ or ABZ-NCs, as well as DMNs delivering coarse ABZ as indicated by the relative bioavailability values of >100%. Therefore, the combination approach developed in this study could maintain the systemic circulation of ABZ, which could be possibly caused by avoiding the first-pass metabolism in the liver. This could be beneficial to improve the efficacy of ABZ in CE treatment.

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“…NCs are drug nanoparticles with crystalline features, with minimal carrier materials or excipients, therefore capable of attaining a drug loading of close to 100% [151]. The term nanosuspension refers to the NCs dispersed in a liquid, whereas solid and re-dispersible NCsbased powders can be obtained by solvent removal [152][153][154][155]. NCs can be produced by two main approaches, "bottom-up" techniques, which consists of controlled drug precipitation from a solution, or by "top-down" techniques, which include the application of external shear forces [156].…”

Section: Nano/micro Drug Crystals Loaded Mnmentioning

confidence: 99%

Microneedle array systems for long-acting drug delivery

Vora

Moffatt

Tekko

et al. 2021

European Journal of Pharmaceutics and Biopharmaceutics

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Ricobendazole nanocrystals obtained by media milling and spray drying: Pharmacokinetic comparison with the micronized form of the drug

Cited by 55 publications

References 39 publications

3D-printed implantable devices with biodegradable rate-controlling membrane for sustained delivery of hydrophobic drugs

3D-printed implantable devices with biodegradable rate-controlling membrane for sustained delivery of hydrophobic drugs

Albendazole Nanocrystal-Based Dissolving Microneedles with Improved Pharmacokinetic Performance for Enhanced Treatment of Cystic Echinococcosis

Microneedle array systems for long-acting drug delivery

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