Mucoadhesive buccal disks for novel nalbuphine prodrug controlled delivery: effect of formulation variables on drug release and mucoadhesive performance.
The objective of this work was to assess the effects of drug solubility and loading percent, as well as Carbopol 934/hydroxypropylcellulose (CP/HPC) ratio, on drug release and mucoadhesive performance of the nalbuphine prodrug loaded buccal disks. Drug release rates for the disks were found to be a function of drug solubility, with higher drug release rates for disks loaded with more hydrophilic prodrugs and an increased amount of beta-cyclodextrin. The drug release rates increased with loading percents for nalbuphine hydrochloride, whereas an opposite drug release trend was observed for disks loaded with nalbuphine enanthate, which can be explained by the diffusional drug release mechanism. The CP/HPC ratio affected release rates of nalbuphine enanthate, whereas the ratio had no impact on the release of nalbuphine hydrochloride. Within the 2 days of experiment time, all formulations attached well to the porcine buccal tissues, indicating those formulation variables had no influence on the mucoadhesive performance of CP/HPC-based buccal disks.
Han
R Y
RY
Department of Pharmacy, Chia-Nan College of Pharmacy and Science, Tainan Hsien, Taiwan, ROC.
Fang
J Y
JY
Sung
K C
KC
Hu
O Y
OY
D000180:Acrylic Resins; D000818:Animals; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D066298:In Vitro Techniques; D009061:Mouth Mucosa / Q000502:physiology; D009266:Nalbuphine / Q000493:pharmacokinetics*; D011145:Polyvinyls / Q000737:chemistry*; D011480:Protease Inhibitors / Q000737:chemistry; D012995:Solubility; D013552:Swine; D000267:Tissue Adhesions
D000180:Acrylic Resins; D011145:Polyvinyls; D011480:Protease Inhibitors; C006912:carboxypolymethylene; D002482:Cellulose; C008079:hydroxypropylcellulose; D009266:Nalbuphine