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. 2021 Jul 2:15:2869-2884.
doi: 10.2147/DDDT.S309078. eCollection 2021.

Superhydrophobic Surface for Enhancing the Bioavailability of Salbutamol Sulfate from Cross-Linked Microspheres: Formulation, Characterization, and in vivo Evaluation

Dalia Gaber  1 , Siham Abdoun  1 , Ameerah Alfuraihy  2 , Bushra Altasan  2 , Amal Alsubaiyel  1
Affiliations

Superhydrophobic Surface for Enhancing the Bioavailability of Salbutamol Sulfate from Cross-Linked Microspheres: Formulation, Characterization, and in vivo Evaluation

Dalia Gaber et al. Drug Des Devel Ther. .

Abstract

Introduction: The aim of the work was to formulate salbutamol sulfate (SB) microspheres by using superhydrophobic surface (SHS) under different processing factors for improving its encapsulation efficiency, controling its release rate, and hence enhancing its bioavailability.

Methods: Cross-linked microspheres of chitosan (CN) and carrageenan (KN) were made on a SHS under a glutaraldehyde-saturated atmosphere. The formulations were designed and optimized based on 42 factorial design. Percentage encapsulation efficiency (%EE), particle size, swelling ratio, and in vitro release rate were characterized, and the in vivo performance of optimized formula was investigated in beagle dogs.

Results: The results showed that the prepared microspheres have a high %EE (97.11±0.78%) for F13. The swelling ratio was 4.2 at the end of the 8 hours for the optimized formula, and the in vitro release rate was controlled for 12 hours. In vivo study verified that there was a 1.61-fold enhancement in SB bioavailability from optimized formula (F13) compared to market tablet.

Conclusion: The study suggested that microspheres prepared from CN/KN crosslinking on an SHS using glutaraldehyde atmosphere is a promising technique that can encapsulate and sustain the release of water-soluble drugs such as SB in addition to improving its in vivo pharmacokinetic profile.

Keywords: bioavailability; cross-linked complex; microspheres; salbutamol sulfate; superhydrophobic; sustain release; water-soluble drugs.

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Conflict of interest statement

The authors declare no conflicts of interest for this work.

Figures

Figure 1
Figure 1
(A) Chemical structure of chitosan (CN), (B) chemical structure of carrageenan (KN).
Figure 2
Figure 2
Chemical structure of salbutamol sulfate (SB).
Figure 3
Figure 3
SEM images of the prepared superhydrophobic surface (the magnification power 25,000×, 100,000×)ss.
Figure 4
Figure 4
Images show contact angles for (A) water, (B) CN, (C) SB-CN-based dispersion, and (D) SB-CN/KN-based dispersion droplets on SHS.
Figure 5
Figure 5
Scanning image of F13 microsphere formula.
Figure 6
Figure 6
Line plot for the effect of (A) drug-to-polymer ratio, (B) dropper tip size, (C) dropping distance, and (D) duration of crosslinking on the encapsulation efficiency (%EE) of SB-CN microspheres.
Figure 7
Figure 7
DSC thermogram of pure salbutamol sulfate SB, chitosan CN, carrageenan, and optimized formula F13.
Figure 8
Figure 8
FTIR spectra of CN, KN, CN/KN microspheres dispersion, SB, and F13.
Figure 9
Figure 9
Digital image of swollen SB microspheres (F13) after immersing in 0.1N HCl for 2 hours then in phosphate buffer up to 8 hours.
Figure 10
Figure 10
Swelling ratios of SB microspheres (F1, F3, F5, F7, F9, F11, F13, and F15) in 0.1N HCl for 2 hours then phosphate buffer (pH 6.8) up to 8 hours.
Figure 11
Figure 11
(A) In vitro dissolution profiles of SB from SBTs for F1–F8 in 0.1N HCl for two hours followed by phosphate buffer up to 24 hours. (B) In vitro dissolution profiles of SB from SBTs for F9–F16 in 0.1N HCl for two hours followed by phosphate buffer up to 24 hours.
Figure 12
Figure 12
Mean (±SE) plasma SB concentrations following oral administration of commercial tablets and F13 tablets to six beagle dogs.
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