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Sains Malaysiana 53(10)(2024): 3445-3454
http://doi.org/10.17576/jsm-2024-5310-17
Solubility and
Dissolutıon Improvement of Paramethoxycinnamic Acid (PMCA) Induced by
Cocrystal Formation using Caffeine as a Coformer
(Penambahbaikan Keterlarutan dan Pelarutan Asid
Parametoksisinamik (PMCA) Teraruh oleh Pembentukan Kokristal menggunakan Kafein
sebagai Koformer)
MELANNY IKA
SULİSTYOWATY1, SUCİATİ FİTRİ1,
NİNİS YULİATİ1,2, TAHTA AMRİLLAH3,
CHE AZURAHANİM CHE ABDULLAH4 & DWİ SETYAWAN1,*
1Department
of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga,
Surabaya 60115, Indonesia
2Department of Pharmacy Technology, Faculty of Pharmacy, Institut Ilmu
Kesehatan Bhakti Wiyata Kediri, Kediri 64114, Indonesia
3Nanotechnology
Engineering, Faculty of Advanced Technology and Multidiscipline,
Universitas Airlangga, Surabaya 60115, Indonesia
4Institute of Nanoscience and Nanotechnology, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia
Received: 21 August 2023/Accepted: 13 August 2024
Abstract
Para-methoxy cinnamic acid (pMCA) is a derivative
compound of ethyl p-methoxycinnamate that could be obtained in nature. pMCA has
excellent pharmacological properties. However, in their application as a drug,
pMCA has poor water solubility. In this present research, we try to increase
the water solubility of pMCA using the cocrystal formation (cocrystallization)
strategy. Here, we use caffeine as a coformer that can interact very well with
pMCA via non-covalent bonding and Van der Waals interaction to achieve
cocrystal formation. The cocrystal samples were successfully synthesized using
various synthesis techniques; physical mixture, solvent evaporation, and
microwave radiation methods. It shows that the solubility of the
samples synthesized using microwave-assisted and solvent evaporation increases
about 3.30 and 3.12 times, respectively, whereas the dissolution rate profile
increases 2.50 and 2.39 times, respectively, compared to pure APMS. Our findings explain the importance of the cocrystal formation
strategy to enhance the solubility of active material pMCA. This strategy can
also be used as a standard formulation of a new drug system with excellent
solubility and dissolution which is very important for the pharmaceutical
industry.
Keywords: Caffeine; cocrystal; dissolution; drugs;
para-methoxy cinnamic acid; solubility
Abstrak
Asid sinamik para-metoksi (pMCA) ialah sebatian
terbitan etil p-metoksisinamat yang boleh didapati secara semula jadi. pMCA
mempunyai sifat farmakologi yang sangat baik seperti sifat analgesik,
anti-radang, anti-diabetes, anti-kanser, hepatopelindung dan neuropelindung.
Walau bagaimanapun, dalam penggunaannya sebagai ubat, pMCA mempunyai
keterlarutan air yang lemah. Manakala, keterlarutan dadah merupakan aspek
penting yang perlu dimiliki oleh sesuatu ubat untuk mencapai kesan yang
dikehendaki. Dalam penyelidikan ini, kami cuba meningkatkan keterlarutan air
pMCA menggunakan strategi pembentukan kokristal (penghabluran). Di sini, kami
menggunakan kafein sebagai koformer yang boleh berinteraksi dengan baik dengan
pMCA melalui ikatan bukan kovalen dan interaksi Van der Waals untuk mencapai
pembentukan kokristal. Sampel kokristal telah berjaya disintesis menggunakan
pelbagai teknik sintesis; campuran fizikal, penyejatan pelarut dan kaedah
sinaran gelombang mikro. Semua sampel kokristal mempunyai keterlarutan yang sangat
baik berbanding dengan keadaan murni atau pMCA tulen. Sampel yang disediakan
menggunakan sinaran gelombang mikro mempunyai keterlarutan yang paling tinggi
berbanding sampel yang disediakan menggunakan kaedah campuran fizikal dan
penyejatan pelarut. Penemuan kami menerangkan kepentingan strategi pembentukan
kokristal untuk meningkatkan keterlarutan bahan aktif pMCA. Strategi ini juga
boleh digunakan sebagai formulasi standard sistem ubat baharu dengan
keterlarutan dan pembubaran yang sangat baik yang sangat penting untuk industri
farmaseutikal.
Kata kunci: Asid sinamik para-metoksi; dadah;
kafein; keterlarutan; kokristal; pembubaran
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*Corresponding
author; email: dwisetyawan-90@ff.unair.ac.id
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