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Peer-reviewedCC BY 4.0Polymers

Probing Melatonin’s Release Pattern from Oral Solid Dosage Forms Using Synthetic Biopolymers

  • Angeliki Siamidi1
  • Nikolaos Bikiaris2
  • Chrystalla Protopapa1
  • Maria Plyta1
  • Maria Saltou1
  • Aikaterini Sakellaropoulou3
  • Marilena Vlachou1
  1. 1Section of Pharmaceutical Technology, Department of Pharmacy, National and Kapodistrian University of Athens, 15771 Athens, Greece
  2. 2Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, Greece
  3. 3Section of Pharmaceutical Chemistry, Department of Pharmacy, National and Kapodistrian University of Athens, 15771 Athens, Greece
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Abstract

Melatonin (N-acetyl-5-methoxytryptamine) (MLT) is a naturally occurring hormone produced endogenously, primarily in the suprachiasmatic nucleus. MLT exhibits a plethora of uses particularly in the treatment of sleep disorders (sleep onset and maintenance). However, due to its short biological half-life, MLT cannot maintain effective plasma concentrations for a prolonged period when it is exogenously taken from immediate-release formulations. The present study aims at developing modified release systems capable of gradually releasing MLT, thereby sustaining its pharmacological effect over eight hours. To this end, modified-release tablets were prepared using new polymeric excipients based on polylactic acid (PLA). Both neat PLA and PLA copolymers with polyethylene glycols (PEGs) of varying molecular weights (PLLA-PEG-PLLA_4000, PLLA-PEG-PLLA_6000, and PLLA-PEG-PLLA_8000) were used, along with other excipients. Certain formulations delivered MLT comparatively fast and may therefore be useful for sleep onset problems, others matched the release behaviour of the marketed product Circadin®, and the rest released the hormone in a more prolonged manner.

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Cite

BibTeXRIS
BibTeX
@article{siamidi2026probing,
  title = {{Probing Melatonin’s Release Pattern from Oral Solid Dosage Forms Using Synthetic Biopolymers}},
  author = {Angeliki Siamidi and Nikolaos Bikiaris and Chrystalla Protopapa and Maria Plyta and Maria Saltou and Aikaterini Sakellaropoulou and Marilena Vlachou},
  journal = {Polymers},
  year = {2026},
  month = oct,
  doi = {10.3390/polym18202570},
  url = {https://www.mdpi.com/2073-4360/18/20/2570},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - Probing Melatonin’s Release Pattern from Oral Solid Dosage Forms Using Synthetic Biopolymers
AU  - Angeliki Siamidi
AU  - Nikolaos Bikiaris
AU  - Chrystalla Protopapa
AU  - Maria Plyta
AU  - Maria Saltou
AU  - Aikaterini Sakellaropoulou
AU  - Marilena Vlachou
PY  - 2026
DA  - 2026/10/01
JO  - Polymers
DO  - 10.3390/polym18202570
UR  - https://www.mdpi.com/2073-4360/18/20/2570
AB  - Melatonin (N-acetyl-5-methoxytryptamine) (MLT) is a naturally occurring hormone produced endogenously, primarily in the suprachiasmatic nucleus. MLT exhibits a plethora of uses particularly in the treatment of sleep disorders (sleep onset and maintenance). However, due to its short biological half-life, MLT cannot maintain effective plasma concentrations for a prolonged period when it is exogenously taken from immediate-release formulations. The present study aims at developing modified release systems capable of gradually releasing MLT, thereby sustaining its pharmacological effect over eight hours. To this end, modified-release tablets were prepared using new polymeric excipients based on polylactic acid (PLA). Both neat PLA and PLA copolymers with polyethylene glycols (PEGs) of varying molecular weights (PLLA-PEG-PLLA_4000, PLLA-PEG-PLLA_6000, and PLLA-PEG-PLLA_8000) were used, along with other excipients. Certain formulations delivered MLT comparatively fast and may therefore be useful for sleep onset problems, others matched the release behaviour of the marketed product Circadin®, and the rest released the hormone in a more prolonged manner.
SN  - 2073-4360
ER  -