International Journal of Drug Delivery Technology
Volume 16, Issue 4s

Advanced Design and Optimization of Lafutidine-Encapsulated Low-Density Floating Microspheres

Yogita Akash Shinde1, Lalbihari Barik2, Jahnavi Harshil Bhatt3, Aman Sharma4, Alphonsa Mathew5, Swatantr Bahadur Singh6, Farhad F Mehta7, Ketaki Suhas Shinde8*

1Assistant Professor, Vishwakarma University School of Pharmacy Pune, Laxmi Nagar, Kondhwa (Budruk), Pune, Maharashtra 411048
2Associate Professor, Department of Information System, Faculty of Computing and Information Technology in Rabigh, King Abdulaziz University
3Assistant Professor, Parul Institute of Pharmacy, Parul University, P.O. Limda, Ta. Waghodiya, Vadodara, Gujarat - 391760
4Associate Professor, Chandigarh College of Pharmacy, Chandigarh Group of Colleges, Landran, Punjab, India, 140307
5Associate Professor, Indira Gandhi Institute of Pharmaceutical Sciences, Perumbavoor, Asamannoor P. O., Odakkali, 683549
6Assistant Professor, School of Pharmaceutical Sciences, Faculty of Pharmacy, IFTM University, Moradabad, Uttar Pradesh, India 244001
7Assistant Professor, School of Pharmaceutical Sciences, UTD, RGPV University, Bhopal, Madhya Pradesh, Pin 462033
8*Research Scholar, Krishna Institute of Pharmacy, Krishna Vishwa Vidyapeeth (Deemed to be University), Karad 415539; Assistant Professor, KCT's Krishna College of Pharmacy, Karad, Maharashtra 415539

(Corresponding Author)

ABSTRACT

Background: Lafutidine, a potent H₂-receptor antagonist with cytoprotective properties, suffers from poor bioavailability due to its short half-life and narrow absorption window in the upper gastrointestinal tract. Conventional formulations release the drug rapidly, leading to fluctuating plasma levels and reduced therapeutic efficacy. To overcome these limitations, a gastroretentive floating microsphere system was designed and optimized to enhance gastric residence time and sustain drug release.

Methods: Lafutidine floating microspheres were prepared by the solvent evaporation method using a polymer blend of hydroxypropyl methylcellulose (HPMC K4M), ethyl cellulose, and Eudragit S100. A 3² factorial design was employed to study the effects of polymer-to-drug ratio and stirring speed on critical responses, including particle size, entrapment efficiency, buoyancy, and cumulative drug release. The formulations were characterized for morphology (SEM), drug loading, buoyancy, in vitro dissolution in 0.1 N HCl (pH 1.2), and release kinetics modeling.

Results: Particle size varied from 176.2 ± 3.8 to 310.6 ± 6.7 µm, with entrapment efficiency ranging between 68.5 ± 2.1% and 91.2 ± 1.8%. Optimized formulations (F5 and F6) exhibited spherical, porous morphology, high entrapment efficiency (>85%), and excellent buoyancy (>90% for 12 h). In vitro release was sustained for 12 h, with 82.5 ± 2.7% (F5) and 80.4 ± 2.5% (F6) cumulative release, following Higuchi kinetics (R² > 0.98) and anomalous non-Fickian diffusion (n = 0.58–0.61). Comparative evaluation confirmed superior gastric retention and predicted oral bioavailability (~55–60%) over marketed tablets and previously reported gastroretentive systems.

Conclusion: The study establishes Lafutidine-loaded floating microspheres as a promising gastroretentive delivery system, capable of enhancing gastric residence, sustaining release, and improving therapeutic efficiency in acid-related disorders. Future in vivo studies are warranted to validate clinical translation and scale-up potential.

Keywords: Lafutidine, floating microspheres, gastroretentive drug delivery, solvent evaporation, factorial design, sustained release.

How to cite this article: Shinde YA, Barik L, Bhatt JH, Sharma A, Mathew A, Singh SB, Mehta FF, Shinde KS, Advanced Design and Optimization of Lafutidine-Encapsulated Low-Density Floating Microspheres. Int J Drug Deliv Technol. 2026;16(4s): 813-820; DOI: 10.25258/ijddt.16.4s.94

Source of support: Nil

Conflict of interest: None