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Carrageenan-Acyclovir Complex and Its Liposomal Form
Irina M Yermak1, Valery P Glazunov1, Natalya V Krylova2
1G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences (FEB RAS), 100 Let Vladivostoku Prosp. 159, 690022 Vladivostok, Russia.
Carrageenans (CRGs) from Chondrus armatus form complexes with acyclovir (ACV), enhancing its antiviral activity against herpes simplex virus (HSV-1). This CRG/ACV complex, especially in liposomes, shows improved mucoadhesion and prophylactic effects with reduced drug dosage.
Area of Science:
- Pharmacology
- Biochemistry
- Materials Science
Background:
- Carrageenans (CRGs) are sulfated polysaccharides with potential applications in drug delivery.
- Acyclovir (ACV) is a common antiviral medication.
- Developing effective drug delivery systems is crucial for improving antiviral therapy.
Purpose of the Study:
- To develop and characterize a mucoadhesive complex of carrageenans (CRGs) and acyclovir (ACV).
- To evaluate the antiviral efficacy and prophylactic effects of the CRG/ACV complex against herpes simplex virus (HSV-1).
- To investigate the potential of liposomal formulations of the CRG/ACV complex for enhanced antiviral delivery.
Main Methods:
- Complex formation between CRGs and ACV was confirmed using IR spectroscopy and quantum-chemical calculations.
- ζ-potential distribution was analyzed to confirm complex formation.
- Antiviral activity was assessed by evaluating the inhibition of cytopathic effects of HSV-1 on host cells.
- Liposomal formulations of the CRG/ACV complex were prepared and characterized.
Main Results:
- CRGs and ACV formed complexes via hydrogen bonding and coordination interactions with an enthalpy of 15-20 kcal/mol.
- The CRG/ACV complex demonstrated enhanced antiviral activity, allowing for reduced ACV dosage and exhibiting prophylactic effects.
- Liposomal CRG/ACV complex showed significant mucoadhesion, potent antiviral activity (SI 344), and a heightened prophylactic effect (SI 128).
Conclusions:
- CRG/ACV complexes represent a promising approach for developing effective antiviral therapies.
- Liposomal encapsulation further enhances the mucoadhesive and antiviral properties of the CRG/ACV complex.
- These novel compounds selectively inhibit viral adsorption and replication without harming host cells.
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