Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
The purpose of the present work was to develop nanoemulsion-based formulations of mirtazapine for intranasal delivery using a spray actuator to target the brain for treating depression. Research on the solubility of medications in different oils, surfactants, co-surfactants, and solvents has been done. Using pseudo-ternary phase diagrams, the various ratios of the surfactant and co-surfactant mix were computed. Thermotriggered nanoemulsion was formulated using different concentrations of poloxamer 407 (i.e., 15%, 15.5%, 16%, 16.5% up to 22%). Similarly, mucoadhesive nanoemulsion using 0.1% Carbopol and water-based plain nanoemulsions were also prepared for comparative assessment. The developed nanoemulsions were analyzed for physicochemical properties, i.e., physical appearance, pH, viscosity, and drug content.
Drug-excipient incompatibility was determined by Fourier transform infrared spectral (FTIR) analysis and differential scanning calorimetry (DSC). In vitro drug diffusion studies were conducted for optimized formulations. Among the three formulations, RD1 showed the highest percentage of drug release. Ex vivo drug diffusion studies were conducted on freshly excised sheep nasal mucosa with Franz diffusion cell simulated nasal fluid (SNF) for all three formulations up to 6 h, and the thermotriggered nanoemulsion (RD1) showed 71.42% drug release with 42.64 nm particle size and a poly dispersity index of 0.354. The zeta potential was found to be −6.58. Based on the above data, it was concluded that thermotriggered nanoemulsion (RD1) has great potential to be used as an intranasal gel for treating depression in patients. It can offer great benefits by reducing dosing frequency and improving bioavailability of mirtazapine by direct nose-to-brain delivery.
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Materials
Mirtazapine (CAS: 85650-52-8) was procured as a kindly gifted sample from Wockhardt Pvt. Ltd., Aurangabad, Maharashtra, India. Poloxamer 407 (Kolliphor P 407) (CAS: 691397-13-4) was obtained as a gifted sample from BASF India, Ltd., Mumbai, India. Labrafil M1944 CS (CAS: 69071-70-1), Capryol PGMC (CAS: 31565-12-5), Peceol, and Labrosol, were gift samples from Gattefosse India, Pvt. Ltd. (Mumbai, India), while Capmul MCM C8 EP (CAS: 26402-26-6) and Acconon MC82E/NF (CAS: 85536-01-8) were a generous gifts from Abitech Ltd. Finar Chemicals, Hyderabad, India supplied the Tween 80, Tween 20, Span 80, propylene glycol, polyethylene glycol 400, and oleic acid. The remaining reagents were all of analytical grade.
Ghazwani, M.; Vasudevan, R.; Kandasamy, G.; Manusri, N.; Devanandan, P.; Puvvada, R.C.; Veeramani, V.P.; Paulsamy, P.; Venkatesan, K.; Chidmabaram, K.; Dhurke, R. Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug. Gels 2023, 9, 457. https://doi.org/10.3390/gels9060457
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