DEVELOPMENT AND EVALUATION OF NEBIVOLOL
HYDROCHLORIDE NANOCRYSTALS IMPREGNATED BUCCAL FILM
BANDAR E AL-DHUBIAB 1*, ANROOP B NAIR 1, RACHNA KUMRIA 2, MAHESH ATTIMARAD 1, SREE HARSHA 1
1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi
Arabia
2Swift School of Pharmacy, Village-Ghaggar Sarai, Rajpura, Patiala, Punjab, India
*corresponding author: baldhubiab@kfu.edu.sa
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Abstract:
Clinical efficacy of nebivolol is restricted primarily because of its low aqueous solubility and extensive hepatic metabolism. This
study investigated the prospective of enhancing the systemic delivery of nebivolol HCl by formulating nanocrystals impregnated
films for the buccal application. Nanocrystals of nebivolol HCl were prepared by acid-base neutralization method. Placebo films
(N1-N3) were optimized by varying concentrations of chitosan. Further pure nebivolol HCl and its nanocrystals were
incorporated to the films at two levels (2.5 mg/cm2 and 5 mg/cm2). The prepared films (N4-N7) were assessed for
physicomechanical properties, swelling, drug release and permeation by standard protocols. Selected films were evaluated in
vivo on rabbits. Physicomechanical properties displayed by the prepared films (N4-N7) were found to be adequate for the
buccal application. Rapid swelling of films was noticed which would be beneficial and may contribute to immediate and
effective bioadhesion with the buccal mucosa. The rate of drug dissolution was rapid and complete in 4 h from nanocrystals
embedded films (N6 and N7) when compared to films loaded with pure drug. The permeation data indicates greater transport
when drug concentration was higher (Film N7; 36.31 ± 6.54 μg/cm2/h; p < 0.0001). In vivo data signified rapid absorption
(Cmax ~ 24 ng/mL) and higher AUC0-α (~4 00 ng * h/mL) with ~ 2.5 folds improvement in the bioavailability. In conclusion,
registered data suggests that the buccal application of nanocrystals embedded film improved the efficacy of nebivolol HCl,
and necessitates further clinical studies.






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