Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis

Sim, Jeeho; Kang, Geonwoo; Yang, Hyung Kook; Jang, Mingyu; Kim, You-Seong; Ahn, Hyeri; Kim, Minkyung; Jung, Hyungil

doi:10.3390/polym14194027

Cited by 9 publications

(6 citation statements)

References 54 publications

(65 reference statements)

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“…The addition of trehalose to the formulation considerably improved the drug stability. Furthermore, the needles rapidly delivered 87.6% of the drug into porcine skin after 5 min [ 213 ]. An investigation by Zhou et al demonstrated the successful fabrication of dissolving microneedles from a natural material (Bletilla striata polysaccharide).…”

Section: Microneedle Types For Biopharmaceutical Deliverymentioning

confidence: 99%

Microneedle-Mediated Transdermal Delivery of Biopharmaceuticals

Nguyen

2023

Pharmaceutics

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Transdermal delivery provides numerous benefits over conventional routes of administration. However, this strategy is generally limited to a few molecules with specific physicochemical properties (low molecular weight, high potency, and moderate lipophilicity) due to the barrier function of the stratum corneum layer. Researchers have developed several physical enhancement techniques to expand the applications of the transdermal field; among these, microneedle technology has recently emerged as a promising platform to deliver therapeutic agents of any size into and across the skin. Typically, hydrophilic biomolecules cannot penetrate the skin by passive diffusion. Microneedle insertion disrupts skin integrity and compromises its protective function, thus creating pathways (microchannels) for enhanced permeation of macromolecules. Microneedles not only improve stability but also enhance skin delivery of various biomolecules. Academic institutions and industrial companies have invested substantial resources in the development of microneedle systems for biopharmaceutical delivery. This review article summarizes the most recent research to provide a comprehensive discussion about microneedle-mediated delivery of macromolecules, covering various topics from the introduction of the skin, transdermal delivery, microneedles, and biopharmaceuticals (current status, conventional administration, and stability issues), to different microneedle types, clinical trials, safety and acceptability of microneedles, manufacturing and regulatory issues, and the future of microneedle technology.

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Section: Microneedle Types For Biopharmaceutical Deliverymentioning

confidence: 99%

Microneedle-Mediated Transdermal Delivery of Biopharmaceuticals

Nguyen

2023

Pharmaceutics

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“…Therefore, a series of experiments on oral delivery of PTH or long‐acting and slow‐released preparation is being carried out. Including a weekly dose teriparatide encapsulated dissolving microneedle patch, 247 an orally available enteric‐microencapsulated teriparatide‐deoxycholic acid nanocomplex, 248 a triple padlock nanocarrier prepared by a taurocholic acid‐conjugated chondroitin sulfate, 249 and an oleic acid‐based dispersion in combination with chitosan‐teriparatide polyelectrolyte complex, 250 whose efficacy needs further verification.…”

Section: Anti‐osteoporosis Therapiesmentioning

confidence: 99%

Mechanistic advances in osteoporosis and anti‐osteoporosis therapies

Wang

Luo

Wang

et al. 2023

MedComm

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Osteoporosis is a type of bone loss disease characterized by a reduction in bone mass and microarchitectural deterioration of bone tissue. With the intensification of global aging, this disease is now regarded as one of the major public health problems that often leads to unbearable pain, risk of bone fractures, and even death, causing an enormous burden at both the human and socioeconomic layers. Classic anti‐osteoporosis pharmacological options include anti‐resorptive and anabolic agents, whose ability to improve bone mineral density and resist bone fracture is being gradually confirmed. However, long‐term or high‐frequency use of these drugs may bring some side effects and adverse reactions. Therefore, an increasing number of studies are devoted to finding new pathogenesis or potential therapeutic targets of osteoporosis, and it is of great importance to comprehensively recognize osteoporosis and develop viable and efficient therapeutic approaches. In this study, we systematically reviewed literatures and clinical evidences to both mechanistically and clinically demonstrate the state‐of‐art advances in osteoporosis. This work will endow readers with the mechanistical advances and clinical knowledge of osteoporosis and furthermore present the most updated anti‐osteoporosis therapies.

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“…Undeniably, during the preparation, processes such as drying, may increase the drug loss and reduce the efficacy of the drugs. To maintain the stability, Jeeho Sim et al 87 added trehalose to the HA MNs loaded with teriparatide to form bonds with protein drugs, thus slowing down the protein dynamics. After adding 10% trehalose, the activity of the drugs increases to 75.4 AE 8.3% while the activity is only 59.0 AE 3.6% in the control group.…”

Section: Osteoporosismentioning

confidence: 99%