Nestorone nanosuspension-loaded dissolving microneedles array patch: A promising novel approach for “on-demand” hormonal female-controlled peritcoital contraception

Altuntaş, Ebru; Tekko, Ismaiel A.; Vora, Lalitkumar K.; Kumar, Narender; Brodsky, Rebecca; Chevallier, Olivier; McAlister, Emma; Anjani, Qonita Kurnia; McCarthy, Helen; Donnelly, Ryan F.

doi:10.1016/j.ijpharm.2021.121422

Cited by 32 publications

(18 citation statements)

References 79 publications

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“…In vitro experiments showed that 40% of MN patches dissolve within 10 min and approximately 70% of MNs penetrate and dissolve in the skin within 2 h, which is nearly 2-fold higher than conventional MN patches. An in vitro LNG cumulative release profile showed that the MN patch Poly(vinyl alcohol) (PVA) and poly(vinyl pyrrolidone) (PVP) 2 days [38] Hydroxypropyl methylcellulose (HPMC), and PVA Over 1 week [39] Polymeric biodegradable MN patches Poly(lactic-co-glycolic acid) (PLGA) and polylactic acid (PLA) Over 45 days delivers 75.62 ± 22.79% 10 h after application. In vivo pharmacokinetic studies showed that the patch maximum serum concentration (C max ) was slightly lower than oral administration of an LNG suspension (equal drug amount), but there was not any difference in the time for LNG to reach C max (T max ) between the two groups, indicating that the dissolvable MN patch could serve as an alternative to oral contraceptives [37].…”

Section: Dissolvable Mn Patches For Sustained Release Of Hormonesmentioning

confidence: 99%

Section: Dissolvable Mn Patches For Sustained Release Of Hormonesmentioning

confidence: 99%

“…To achieve long-term contraception using dissolvable MN patches, the Donnelly group [38] combined water-soluble MNs with a nano-formulation to incorporate a nanosuspension of nestorone (NES) in a dissolvable MN patch made of PVA and PVP. In so doing, the in vivo duration of the drug active concentration in vivo for up to 2 days [38]. MNs were fabricated by a twostep casting method, as follows: first casting, the NES and PVA nanosuspension is an aqueous solution in the mold as the MN tips; and second casting, the PVA 50K and PVP mixture as the substrate.…”

Section: Dissolvable Mn Patches For Sustained Release Of Hormonesmentioning

confidence: 99%

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Advances in microneedle patches for long-acting contraception

Jiang

Zeng

Zhang

et al. 2023

Acta Materia Medica

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Despite the advances in contraceptives, there is still a high rate of unintended pregnancies worldwide, due in large part to the lack of effective, convenient, and safe birth control methods. Compared with short-acting contraceptives, approaches that offer long-term pregnancy protection have attracted greater interest because of the reduced dosing frequency and improved patient compliance. As a novel transdermal drug delivery system, the microneedle (MN) patch has been widely used for a variety of biomedical applications, including long-acting contraception, due to unique properties, such as painless self-administration and elimination of biohazardous waste. In this review we provide a systemic review of MN patches that have been utilized for long-term contraception, including dissolvable MN patches, polymeric biodegradable MN patches, and silk fibroin-based biodegradable MN patches. The acceptability and biosafety of these contraceptive MN patches are also discussed. Finally, we give our perspectives on the future clinical translation of MN patches for long-acting contraception.

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Section: Dissolvable Mn Patches For Sustained Release Of Hormonesmentioning

confidence: 99%

Section: Dissolvable Mn Patches For Sustained Release Of Hormonesmentioning

confidence: 99%

Section: Dissolvable Mn Patches For Sustained Release Of Hormonesmentioning

confidence: 99%

See 1 more Smart Citation

Advances in microneedle patches for long-acting contraception

Jiang

Zeng

Zhang

et al. 2023

Acta Materia Medica

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“…Non-invasive and easy self-administration are crucial requirements for on-demand contraceptives, thus MAPs seem an efficient administration strategy for contraceptive drugs delivery. Altuntas et al designed a soluble PVA/PVP-based MAPs for Nestorone ® (NES) nanosuspension-like delivery for "on demand" contraception (Altuntas et al, 2022). NES is a non-androgenic contraceptive that prevents the ovulation at low doses (Kumar et al, 2000).…”

Section: Nanoemulsions and Nanosuspensions: Classical Strategies To F...mentioning

confidence: 99%

Microneedle‐assisted transdermal delivery of nanoparticles: Recent insights and prospects

Guillot

Martínez-Navarrete

Zinchuk-Mironova

et al. 2023

WIREs Nanomed Nanobiotechnol

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Transdermal delivery of drugs offers an interesting alternative for the administration of molecules that present certain troubles when delivered by the oral route. It can produce systemic effects or perform a local action when the formulation exerts an optimal controlled drug release or a targeted delivery to the specific cell type or site. It also avoids several inconveniences of the oral administration such as the hepatic first pass effect, gastric pH-induced hydrolysis, drug malabsorption because of certain diseases or surgeries, and unpleasant organoleptic properties. Nanomedicine and microneedle array patches (MAPs) are two of the trendiest delivery systems applied to transdermal research nowadays. However, the skin is a protective barrier and nanoparticles (NPs) cannot pass through the intact stratum corneum. The association of NPs and MAPs (NPs@MAPs) work synergistically, since MAPs assist NPs to bypass the outer skin layers, and NPs contribute to the system providing controlled drug release and targeted delivery. Vaccination and tailored therapies have been proposed as fields where both NPs and MAPs have great potential due to inherent characteristics. MAPs conception and easy use could allow selfadministration and therefore facilitate mass vaccination campaigns in undeveloped areas with weak healthcare services. Additionally, nanomedicine is being explored as a platform to personalize therapies in such an important field as oncology. In this work we show recent insights that prove the benefits of NPs@MAPs association and analyze the prospects and the discrete interest of the industry in NPs@MAPs, evaluating different limiting steps that restricts NPs@MAPs translation to the clinical practice.

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“…[11][12][13][14][15][16] In a previous study, Donnelly et al developed a dissolving poly(vinyl alcohol) microneedle array for the rapid delivery of Nestorone, which could attain a maximum blood concentration (C max of 32 ± 14 ng mL −1 ) within one hour of skin penetration. 17 In another study, Guo et al used a gelatin/hyaluronic acid particle mixture to load long-acting insulin, which achieved the successful long-term delivery of insulin to address increasing blood glucose levels and effectively reduced fluctuations. 18 The results arose from studies relating to personcentric drug delivery and are encouraging; however, these systems still do not allow the adjustable release behavior of the same drug in one MNP, such as how fast or slow the drug is released, or how much, and do not correspond to the true sense of PDDS.…”

Section: Introductionmentioning

confidence: 99%