22 factorial design-based biocompatible microneedle arrays containing artemether co-loaded with lumefantrine nanoparticles for transepidermal delivery

Pawar, Sandip; Shende, Pravin

doi:10.1007/s10544-020-0476-8

Cited by 21 publications

(9 citation statements)

References 44 publications

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“…Such limitations led to the emergence of an innovative combination therapy approach based on multi-drug delivery nanocarriers with increasing benefits in diverse diseases, notably cancer [34,35]. Although still in an early stage in the treatment of infectious diseases [36], the carrier-mediated multiple drug approach proved promising in the treatment of malaria [37,38].…”

Section: Introductionmentioning

confidence: 99%

Single oral fixed-dose praziquantel-miltefosine nanocombination for effective control of experimental schistosomiasis mansoni

et al. 2020

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Background The control of schistosomiasis has been centered to date on a single drug, praziquantel, with shortcomings including treatment failure, reinfection, and emergence of drug resistance. Drug repurposing, combination therapy or nanotechnology were explored to improve antischistosomal treatment. The aim of the present study was to utilize a novel combination of the three strategies to improve the therapeutic profile of praziquantel. This was based on a fixed-dose nanocombination of praziquantel and miltefosine, an antischistosomal repurposing candidate, co-loaded at reduced doses into lipid nanocapsules, for single dose oral therapy. Methods Two nanocombinations were prepared to provide 250 mg praziquantel-20 mg miltefosine/kg (higher fixed-dose) or 125 mg praziquantel-10 mg miltefosine/kg (lower fixed-dose), respectively. Their antischistosomal efficacy in comparison with a non-treated control and their praziquantel or miltefosine singly loaded counterparts was assessed in murine schistosomiasis mansoni. A single oral dose of either formulation was administered on the initial day of infection, and on days 21 and 42 post-infection. Scanning electron microscopic, parasitological, and histopathological studies were used for assessment. Preclinical data were subjected to analysis of variance and Tukeyʼs post-hoc test for pairwise comparisons. Results Lipid nanocapsules (~ 58 nm) showed high entrapment efficiency of both drugs (> 97%). Compared to singly loaded praziquantel-lipid nanocapsules, the higher nanocombination dose showed a significant increase in antischistosomal efficacy in terms of statistically significant decrease in mean worm burden, particularly against invasive and juvenile worms, and amelioration of hepatic granulomas (P ≤ 0.05). In addition, scanning electron microscopy examination showed extensive dorsal tegumental damage with noticeable deposition of nanostructures. Conclusions The therapeutic profile of praziquantel could be improved by a novel multiple approach integrating drug repurposing, combination therapy and nanotechnology. Multistage activity and amelioration of liver pathology could be achieved by a new praziquantel-miltefosine fixed-dose nanocombination providing 250 mg praziquantel-20 mg miltefosine/kg. To the best of our knowledge, this is the first report of a fixed-dose nano-based combinatorial therapy for schistosomiasis mansoni. Further studies are needed to document the nanocombination safety and explore its prophylactic activity and potential to hinder the onset of resistance to the drug components.

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Section: Introductionmentioning

confidence: 99%

Single oral fixed-dose praziquantel-miltefosine nanocombination for effective control of experimental schistosomiasis mansoni

et al. 2020

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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%

“…Quantification of the substances, drugs, and proteins carried in the devices was performed in 29 studies. The sample preparation procedure consisted of the complete dissolution of the devices in distilled water, buffer, or mixtures with organic solvent and subsequent quantification [64,67]. For devices composed of at least two polymer layers, in which the nanostructured system was located only in the needle, whereas the baseplate was formed by an inert polymeric structure, the studies described the removal of the microneedles with a scalpel and only the needles were dissolved for analysis [33,34,38,51,52,68,69].…”

Section: Drug or Protein Contentmentioning

confidence: 99%

“…(3) physicochemical characterization of the inserted nanostructured systems and the MN characteristics; (4) protein/nucleotide stability after insertion into the MN; (5) physicochemical characterization of the nanostructured systems and protein/nucleotide stability after insertion into the MN. In all, 27 out of 72 studies measured one of the categories, and of these, only three followed the International Conference on Harmonization (ICH) guideline for stability studies regarding storage conditions: (a) long-term stability (25 ± 2 • C/60% RH ± 5%), (b) accelerate stability (40 ± 2 • C/75% RH ± 5%) [64], and (c) short-term stability (30 ± 2 • C/60% RH ± 5%) [77,78].…”

Section: Stability 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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“…Artemether (ART) and lumefantrine (LUM) are the standard treatment of choice for malaria but possess certain limitations like hydrophobicity and have low oral bioavailability. 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 ).…”

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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22 factorial design-based biocompatible microneedle arrays containing artemether co-loaded with lumefantrine nanoparticles for transepidermal delivery

Cited by 21 publications

References 44 publications

Single oral fixed-dose praziquantel-miltefosine nanocombination for effective control of experimental schistosomiasis mansoni

Single oral fixed-dose praziquantel-miltefosine nanocombination for effective control of experimental schistosomiasis mansoni

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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