TY - JOUR
T1 - Personalised 3D printed Mucoadhesive Gastroretentive Hydrophilic Matrices for Managing Overactive Bladder (OAB)
AU - Khizer, Zara
AU - Akram, Muhammad Rouf
AU - Tahir, Muhammad Azam
AU - Liu, Weidong
AU - Lou, Shan
AU - Conway, Barbara
AU - Ghori, Muhammad Usman
PY - 2023/2/20
Y1 - 2023/2/20
N2 - Overactive bladder (OAB) is a symptomatic complex condition characterised by frequent urinary urgency, nocturia, and urinary incontinence with or without urgency. Gabapentin is an effective treatment for OAB, but its narrow absorption window is a concern, as it is preferentially absorbed from the upper small intestine, resulting in poor bioavailability. We aimed to develop an extended release, intragastric floating system to overcome this drawback. For this purpose, plasticiser-free filaments of PEO (polyethylene oxide) and the drug (gabapentin) was developed using hot melt extrusion. The filaments were extruded successfully with 98% drug loading, possessed good me-chanical properties, and successfully produced printed tablets using FDM (fused deposition modelling). Tablets were printed with varying shell numbers and infill density to investigate their floating capacity. Among seven matrix tablet formulations, F2 (2 shells, 0% infill) showed the highest floating time, i.e., more than 10 hours. Drug release rates fell as infill density and shell number increased. However, F2 was the best-performing formulation in terms of floating and re-lease and was chosen for in vivo (pharmacokinetic) studies. The pharmacokinetic findings exhibit improved gabapentin absorption compared to the control (oral solution). Overall, it can be concluded that 3D printing technology is an easy-to-use approach which demonstrated its benefits in developing medicines based on a mucoadhesive gastroretentive strategy, improving the absorption of gabapentin with potential for improved management of OAB.
AB - Overactive bladder (OAB) is a symptomatic complex condition characterised by frequent urinary urgency, nocturia, and urinary incontinence with or without urgency. Gabapentin is an effective treatment for OAB, but its narrow absorption window is a concern, as it is preferentially absorbed from the upper small intestine, resulting in poor bioavailability. We aimed to develop an extended release, intragastric floating system to overcome this drawback. For this purpose, plasticiser-free filaments of PEO (polyethylene oxide) and the drug (gabapentin) was developed using hot melt extrusion. The filaments were extruded successfully with 98% drug loading, possessed good me-chanical properties, and successfully produced printed tablets using FDM (fused deposition modelling). Tablets were printed with varying shell numbers and infill density to investigate their floating capacity. Among seven matrix tablet formulations, F2 (2 shells, 0% infill) showed the highest floating time, i.e., more than 10 hours. Drug release rates fell as infill density and shell number increased. However, F2 was the best-performing formulation in terms of floating and re-lease and was chosen for in vivo (pharmacokinetic) studies. The pharmacokinetic findings exhibit improved gabapentin absorption compared to the control (oral solution). Overall, it can be concluded that 3D printing technology is an easy-to-use approach which demonstrated its benefits in developing medicines based on a mucoadhesive gastroretentive strategy, improving the absorption of gabapentin with potential for improved management of OAB.
KW - 3D printing
KW - Gabapentin
KW - Hydrophilic matrices
KW - Extended drug release
KW - Gastroretention
KW - Mucoadheison
KW - Polyethylene oxide
M3 - Article
JO - Pharmaceuticals
JF - Pharmaceuticals
SN - 1424-8247
ER -