Abstract：
:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of CBZ. The MCC was formulated using interphase, coparticulate–cosolvent homogenization technique, and lyophilization. In vitro, ex vivo, and in vivo investigations were performed. The mesoporous (pore width = 80.1233 Å) MCC was mechanically stable (Є(D) = 0.0290 J, M(F) = 8.5490 N/mm) and resilient (M(R) = 5.5040%). It demonstrated distinctive controlled release (9.9800%/h), permeation enhancing (10.8730%/h), drug loading (90.0541%), and bioadhesive (ω(adh) = 0.0034 J, F(det) = 1.0751 N) capacities. In vivo studies on pigs showed the ability of the MCC to effectively initiate and regulate transbuccal permeation of CBZ as visualized by outcomes of the quantitative and qualitative assessments of isolated plasma samples. Furthermore, comparisons of in vitro and in vivo data of MCC with a conventional product highlighted its capability to attain higher bioavailability and more controlled release trends. Histological and cytological investigations confirmed that the MCC is biocompatible. The mathematical model produced relevant pharmacokinetics and in vitro/in vivo correlation information.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Adeleke OA,Choonara YE,Du Toit LC,Pillay Vdoi
10.1002/jps.23884subject
Has Abstractpub_date
2014-04-01 00:00:00pages
1157-69issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)30633-Xjournal_volume
103pub_type
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