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Mucoadhesive (Type-I) and Floating (Type-II) Chitosan Beads for Improved Gastric Retention of Clarithromycin

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Abstract

Purpose

Floating drug delivery systems present one of the effective strategies to treat gastric disorders including peptic ulcer. To improve the retention of Clarithromycin at the target site of H. pylori induced ulcer, the current study undertakes development of gastro-retentive drug delivery systems based on muco-adhsesion (type I) and floating (type II) properties of the beads.

Method

Two different types of beads were prepared by ionic gelation method. The type-I beads comprised of chitosan and tripolyphosphate (TPP) while the type-II beads contain chitosan and xanthan gum to promote floating properties. The prepared beads were analyzed for size, morphology, circularity, roughness, drug content and association efficiency. The drug release profile of the beads was determined by USP Type II method. The floating capabilities of the beads were confirmed by using floating lag and total floating time. The swelling of the beads was evaluated using water bath at an agitation speed of 100 revolutions per minute. The in-vitro evaluation of muco-adhesion was determined using the fresh chicken eggshell membranes.

Results

The beads ranged in size from 1.9 to 3.0 mm. The size of type-II beads (F3 and F4) was significantly higher than type-I (F1 and F2) beads. The beads of formulations containing higher concentration of polymer (F1 and F2) were more circular while the roughness of type-II beads was significantly higher than type-I (p ≤ 0.05). The association efficiency ranged from 92.67 ± 5.42 to 95.97 ± 2.28% for type-I and type-II beads respectively. The type-I beads have shown sustained drug release in comparison to type-II beads due to compact nature. The type-II beads float within half a minute with total floating time of about 10 h. The type-II beads achieved significantly higher swelling than type-I beads, while the mucoadhesive property of F1 and F2 was significantly higher due to the presence of chitosan.

Conclusion

The study reports two types of beads that can be effectively utilized in H-pylori induced peptic ulcer using improved gastric drug retention via mucoadhesive (type-I) and floating (type-II) characteristics.

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Data Availability

All the relevant data had been included in the manuscript.

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Authors and Affiliations

  1. Particle Design and Drug Delivery Laboratory, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Khyber Pakhtunkhwa, Pakistan

    Habib Ur Rehman, Muhammad Danish Saeed, Faqir Ullah, Faiqa Falak Naz, Kamran Ahmad Khan & Kifayat Ullah Shah

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  1. Habib Ur Rehman
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  2. Muhammad Danish Saeed
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  3. Faqir Ullah
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  4. Faiqa Falak Naz
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  6. Kifayat Ullah Shah
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All the authors have equally contributed in the preparation of final manuscript.

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Correspondence to Kifayat Ullah Shah.

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Rehman, H.U., Saeed, M.D., Ullah, F. et al. Mucoadhesive (Type-I) and Floating (Type-II) Chitosan Beads for Improved Gastric Retention of Clarithromycin. J Pharm Innov 18, 2098–2109 (2023). https://doi.org/10.1007/s12247-023-09776-9

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