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Formulation Options for Mucoadhesive Dosage Forms for Use in the Oral Cavity


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Mucoadhesive polymers used in mucoadhesive buccal film formulations identified in the literaturea

Mucoadhesive polymer Application in mucoadhesive buccal films – API Used plasticizer(s)
Methyl cellulose (MC) Cetylpyridinium chloride, carvedilol, omeprazole, nebivolol Propylene glycol, PEG-400
Ethyl cellulose (EC) Allantoin, fluticasone propionate, propranolol hydrochloride, ketorolac tromethamine, resveratrol, propranolol hydrochloride & nifedipine PEG-400, triethyl citrate, propylene glycol, PEG-800, PEG-600, castor oil, glycerol, dibutylphthalate
Hydroxypropyl methyl cellulose (HPMC) Cetylpyridinium chloride, carvedilol, omeprazole, allantoin, fluticasone propionate, propranolol hydrochloride, ketorolac tromethamine, enalapril maleate, glibenclamide, cetirizine dihydrochloride, glimepiride, nitrendipine, clotrimazole, lidocaine hydrochloride, ibuprofen, ondansetron hydrochloride, meloxicam, prednisolone, rizatriptan benzoate, lycopene, risedronate sodium, clinidipine, furosemide, domperidone, catechin, lidocaine hydrochloride & benzydamine hydrochloride & N-acetyl-l-cysteine, nebivolol, nicotine, piroxicam Propylene glycol, PEG-400, triethyl citrate, PEG-800, PEG-600, castor oil glycerol, PEG-3350, triethanolamine, sorbitol, PEG-200
Hydroxypropyl cellulose (HPC) Ketorolac tromethamine, resveratrol, nitrendipine, clotrimazole, lidocaine hydrochloride, diltiazem hydrochloride, indomethacin, lycopene Propylene glycol, PEG-400, glycerol, PEG-3350
Hydroxyethyl cellulose (HEC) Cetylpyridinium chloride, allantoin, propranolol hydrochloride, meloxicam, moxifloxacin hydrochloride & clove oil, acyclovir, hyaluronic acid, nebivolol PEG-400, triethyl citrate, PEG-600, castor oil, glycerol propylene glycol
Carboxymethyl cellulose (CMC, SCMC) Allantoin, fluticasone propionate, ketorolac tromethamine, enalapril maleate, nitrendipine, ibuprofen, meloxicam, diltiazem hydrochloride, lysozyme, rizatriptan benzoate, ciprofloxacin, glipizide, carvedilol, lycopene, lidocaine hydrochloride & benzydamine hydrochloride & N-acetyl-L-cysteine, simvastatin, lysozyme & epidermal growth factor, imiquimod PEG-400, triethyl citrate, propylene glycol, PEG-800, glycerol, triethanolamine, sorbitol
Xyloglucan (XYL) Rizatriptan benzoate Glycerol
Polycarbophil (PCP) Lidocaine hydrochloride, ibuprofen Glycerol, PEG-3350, triethanolamine, propylene glycol
Polyethylene oxide (PEO) Lidocaine hydrochloride, streptomycin & diclofenac, rizatriptan benzoate, domperidone PEG-3350, glycerol
Poloxamer (POL) Glimepiride, ibuprofen, methylene blue Propylene glycol, PEG-600, glycerol
Polyacrylic acid (PAA) Carvedilol, fluticasone propionate, ketorolac, tromethamine, glimepiride, nitrendipine, clotrimazole, ibuprofen, rizatriptan benzoate, atenolol, prednisolone, lycopene, piroxicam, glipizide Propylene glycol, PEG-800, glycerol, triethanolamine, PEG-400
Polymethacrylic acid (PMA) Carvedilol, glibenclamide, glimepiride, clotrimazole, ibuprofen, acyclovir, penciclovir, almotriptan, prednisolone, glipizide, rizatriptan benzoate Propylene glycol, triethanolamine, PEG-400, PEG-200
Chitosan (CHT) Cetylpyridinium chloride, fluticasone propionate, propranolol hydrochloride & nifedipine, propranolol hydrochloride, ondansetron hydrochloride, tenoxicam, tramadol, progesterone, insulin, lidocaine hydrochloride, clotrimazole, paracetamol, metronidazole, miconazole nitrate, risedronate sodium, lidocaine hydrochloride & benzydamine hydrochloride & N-acetyl-l-cysteine, ropinirole hydrochloride, piroxicam Propylene glycol, PEG-800, glycerol, dibutylphthalate, PEG-400, sorbitol
Polyvinyl alcohol (PVA) Cetylpyridinium chloride, nitrendipine, meloxicam, methylene blue, benznidazole, dexamethasone, paracetamol, rizatriptan benzoate, carvedilol, propranolol hydrochloride, allantoin, propranolol Glycerol, PEG-400, propylene glycol, sorbitol, triethyl citrate, PEG-600, castor oil
Polyvinylpyrrolidone (PVP) Hydrochloride, ketorolac tromethamine, enalapril maleate, nitrendipine, ibuprofen, methylene blue, penciclovir, ondansetron hydrochloride, tenoxicam, tramadol, progesterone, lysine clonixinate, carvedilol, lycopene, simvastatin, ropinirole hydrochloride, epidermal growth factor & lysozyme Glycerol, triethanolamine, propylene glycol
Gelatin (GEL) Ondansetron hydrochloride, lysozyme, progesterone, propranolol hydrochloride, lidocaine hydrochloride Glycerol
Sodium alginate (SA) Cetylpyridinium chloride, omeprazole, cetirizine dihydrochloride, nitrendipine, ciprofloxacin, atenolol, nicotine, carvedilol, lycopene PEG-400, glycerol, propylene glycol
Gellan gum (GLG) Moxifloxacin hydrochloride & clove oil, triamcinolone, acetonide, fluconazole Glycerol, propylene glycol
Guar gum (GUG) Lysine clonixinate, zolmitriptan succinate, α-casozepine Propylene glycol, glycerol
Xanthan gum (XG) Domperidone Not stated
Carrageenan (CRG) Omeprazole, streptomycin & diclofenac, ibuprofen, miconazole nitrate PEG-400, glycerol, PEG-600, propylene glycol
Pectin (PCT) Meloxicam, clotrimazole, paracetamol, metronidazole, triamcinolone acetonide PEG-400, glycerol propylene glycol
Hyaluronic acid (HA) Ondansetron hydrochloride, hyaluronic acid, benzydamine hydrochloride PEG-400, glycerol
Rice starch (RS) Lidocaine hydrochloride, diclofenac sodium, paracetamol Glycerol, PEG-400, propylene glycol, sorbitol
Tapioca starch (TS) Lidocaine hydrochloride Glycerol
Arrowroot starch (AS) Glipizide Glycerol
Agarose (AGR) Zolmitriptan succinate Glycerol
Pullulan (PLL) Enalapril maleate, yonkenafil, methylene blue Glycerol, propylene glycol
Maltodextrin (MAL) Methylene blue Propylene glycol

Various techniques used to produce mucoadhesive buccal films (Shipp et al., 2022).

Method Advantages Disadvantages
Solvent casting Simple, reproducible, and established process; industrial solvent casting offers better control over film thickness and polymer concentrations Drug recrystallization after production; changes in film mechanical properties due to plasticizing small molecules; difficult to achieve dose uniformity; potential for entrapped air bubbles; lack of control over film thickness and polymer concentration
Hot melt extrusion Solventless, continuous process, with fewer operations and better content uniformity than solvent casting; ability to incorporate poorly soluble drugs Drug recrystallization after production; swelling of film after leaving the die; limited and specialist excipients required; agglomeration of ingredients; weight variations due to improper flow, problems with chemical stability; not suitable for thermosensitive drugs
Inkjet printing Recrystallization prevented by depositing API onto the film, rather than building API in; mechanical properties of drug-free film retained; able to precisely deposit small volumes of liquids; ability to personalize treatment Requires another process to make the film deposit drug substances onto; primarily applicable where a low dose of active substance is required; nozzle blockage may lead to inaccurate printed dosages
3D printing Continuous process capability, with personalized treatment; compartmentalization can prevent incompatible excipient interactions; increases precision of manufacture; thermosensitive drugs can be used with high loading capacity FDM (fused deposition modelling) filament production by HME (hot melt extrusion) has the same challenges; drying in SSE (semi-solid extrusion) may alter the dimensions of printed objects; only small-scale, nonreproducible manufacture possible; barriers to clinical adoption for this emerging technology
eISSN:
2453-6725
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Inglés
Calendario de la edición:
2 veces al año
Temas de la revista:
Pharmacy, other