Artemether and lumefantrine dissolving microneedle patches with improved pharmacokinetic performance and antimalarial efficacy in mice infected with Plasmodium yoelii

Volpe‐Zanutto, Fabiana; Ferreira, Letícia Tiburcio; Permana, Andi Dian; Kirkby, Melissa; Paredes, Alejandro J.; Vora, Lalitkumar K.; Bonfanti, Amanda Pires; Charlie-Silva, Ives; Rapôso, Catarina; Figueiredo, Mariana C.; Sousa, Ilza Maria de Oliveira; Brisibe, Andi; Costa, Fábio Trindade Maranhão; Donnelly, Ryan F.; Foglio, Mary Ann

doi:10.1016/j.jconrel.2021.03.036

Cited by 48 publications

(20 citation statements)

References 57 publications

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“…The crystallinity of the OLZ powder and implants was assessed using a Miniflex™ X-ray powder diffractometer (Rigaku Corporation, Tokyo, Japan) equipped with Ni-filtered, Cu Kβ radiation, at a current of 15 mA and a voltage of 30 kV as described previously (Volpe-Zanutto et al., 2021 ).…”

Section: Methodsmentioning

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: Methodsmentioning

confidence: 99%

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

et al. 2022

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“…The distribution of the number of studies by characterization technique is detailed in Figure S2. In parallel, few studies characterized the devices with Fourier transform infrared spectroscopy (FTIR, n = 2) [55,64], X-ray diffraction (XRD, n = 2) [55,64], differential scanning calorimetry (DSC, n = 3) [55,64,65], and thermal gravimetric analysis (TGA, n = 2) [65,66] techniques. In comparison, FTIR, XRD, and DSC techniques were applied to nanostructured system characterization (Figure S1) in 11, 12, and 9 studies, respectively.…”

Section: Methods Employed In Quality Controlmentioning

confidence: 99%

“…With reference to the shape and dimensions of the devices, most studies employed molds to obtain pyramidal and conical MNs, with minor exceptions for other shapes such as tantoblade MNs, the design of which was inspired by traditional Japanese Samurai swords formed by two bevels [53], and only three studies did not inform the MN shape. The dimensions of the needles ranged from 323 to 1500 nm in height [50,54] and from 170 to 400 nm in base diameter [42,55], with the most frequent dimensions varying from 600 and 300 nm [19,56,57], respectively. Approximately 75% of the studies did not describe the needle tip diameter, which ranged from 5 to 40 nm [56,58].…”

Section: Characteristics Of Devicesmentioning

confidence: 99%

“…Out of 21 studies, 15 studies evaluated the developed device against controls. The chosen control groups varied among the studies; some applied needle-free patches produced with the same materials, i.e., polymeric films containing the nanostructures [22,49,55,56,87]. Some studies employed micro-needles containing the substances in their free form, i.e., without the presence of nanostructured systems [41,54,69,77].…”

Section: Mechanical Properties In Vitro Assaysmentioning

confidence: 99%

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Dissolving Microneedles Developed in Association with Nanosystems: A Scoping Review on the Quality Parameters of These Emerging Systems for Drug or Protein Transdermal Delivery

2021

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The largest organ of the body provides the main challenge for the transdermal delivery of lipophilic or high molecular weight drugs. To cross the main barrier of the skin, the stratum corneum, many techniques have been developed and improved. In the last 20 years, the association of microneedles with nanostructured systems has gained prominence for its versatility and for enabling targeted drug delivery. Currently, the combination of these mechanisms is pointed to as an emerging technology; however, some gaps need to be answered to transcend the development of these devices from the laboratory scale to the pharmaceutical market. It is known that the lack of regulatory guidelines for quality control is a hindrance to market conquest. In this context, this study undertakes a scoping review of original papers concerning methods applied to evaluate both the quality and drug/protein delivery of dissolving and hydrogel-forming microneedles developed in association with nanostructured systems.

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“…Therefore dissolvable MNs were formulated containing the drug in micro-suspension to enhance the bioavailability and demonstration of MN-LUM proved to be more effective in control transdermal delivery over the oral treatment (Pawar and Shende 2020a ). MNs array was developed by solvent casting method using artemether co-loaded lumefantrine nanoparticles and the study reported complete permeation of array depicting the drug release upto 60–70% with stability of 6 months extending the release to 24 h. Thus, the MNs proved to be more efficient and safer in transepidermal delivery in case of BCS class II and IV drugs compared to oral administration (Volpe- Zanutto et al 2021 ). The pharmacokinetics study of artemether MN and lumefantrine showed the mean residence time was higher thus, prolongs the release of drug in systemic circulation, improved the bioavailability and proved to be a prominent formulation suitable for combinational antimalarial therapy (Pawar and Shende 2020a , b ).…”

Section: Applicationsmentioning

confidence: 99%

Microneedles in diagnostic, treatment and theranostics: An advancement in minimally-invasive delivery system

Amarnani

Shende

2021

Biomed Microdevices

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Graphical abstract Microneedle (MN) technology plays an important role in biomedical engineering for their less intrusive access to the skin due to minimally or painless penetration, enhancement of drug permeability, improvement of detectability of biomolecules in the epidermal and dermal layers with therapeutic efficacy and safety. Furthermore, MNs possess some major disadvantages like difficulty in scale-up technique, variation in drug delivery pattern with respect to external environment of skin, blockage of arrays due to dermal tissues, induction of inflammation or allergy at the site of administration and restriction of dosing range based on the size of active. Additionally, microneedle acts as a transdermal theranostic device for monitoring the physiological parameters in clinical studies. The investigation of drug transfer mechanisms through microneedles includes coat and poke, poke and flow, poke and patch and poke and release method. This review article discusses different categories of microneedles with fabrication methods such as photolithography, laser cutting, 3D printing, etc. in therapeutic applications for treating cancer, diabetes, arthritis, obesity, neurological disorders, and glaucoma. Biosensing devices based on microneedles may detect target analytes directly in the interstitial fluid by penetrating the stratum corneum of the skin and thus microneedles-based devices can be considered as a single tool in diagnostic sensing and therapeutic administration of drugs inside the body. Moreover, the clinical status and commercial availability of microneedle devices are discussed in this review article to offer new insights to researchers and scientists. Continuous monitoring particularly for the determination of blood glucose concentration is one of the most important requirements for the development of next-generation healthcare devices. The aim of this review article focuses mainly on the theranostic applications of microneedles in various medical conditions such as malaria, glaucoma, cancer, etc.

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Artemether and lumefantrine dissolving microneedle patches with improved pharmacokinetic performance and antimalarial efficacy in mice infected with Plasmodium yoelii

Cited by 48 publications

References 57 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

Dissolving Microneedles Developed in Association with Nanosystems: A Scoping Review on the Quality Parameters of These Emerging Systems for Drug or Protein Transdermal Delivery

Microneedles in diagnostic, treatment and theranostics: An advancement in minimally-invasive delivery system

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