Science and Technology of Bioadhesive-Based Targeted Oral Delivery Systems - Pharmaceutical Technology

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Science and Technology of Bioadhesive-Based Targeted Oral Delivery Systems
Novel hydrophobic bioadhesive polymers and dosage designs are now available to effectively achieve tailored release kinetics of a broad range of drugs to meet the clinical needs.


Pharmaceutical Technology
Volume 32, Issue 11, pp. 100-121


Figure 14: Two pulse release profile from the Gabapentin BIOROD system. (ALL FIGURES AND TABLES ARE COURTESY OF THE AUTHOR.)
The BIOROD system (see Figure 13) comprises a longitudinally compressed capsule shape and inner drug core encased in an impermeable bioadhesive cylinder. One of the significant advantages of this system is its flexibility in constructing various designs to allow release kinetics to meet therapeutic goals. Figure 14 shows two pulse-release behaviors of gabapentin from a BIOROD system. The drug released from such a bioadhesive system can be easily adjusted by:
  • Variation of the architecture of the inner core
  • Variation of rate controlling polymers, including type and concentration in the core
  • Inclusion of placebo and barrier layers within the core
  • Variation of bioadhesive coating shell.

Conclusions

The results and overview presented in this article leave no doubt that bioadhesive-based targeted oral delivery systems have the potential to enable many drugs to be delivered at the desired absorption site in a prolonged and tailored manner. The successful fabrication of the bioadhesive system should take into consideration a multitude of aspects of polymer-mucus interactions, preferred site of absorption, drug loading, GI physiology, dosage form size and shape, and contact duration. Though each of these factors plays a critical role, optimization must be performed to give the best performance in all categories. Fabrication of oral bioadhesive formulations for existing drugs potentially provides access to new and expanded markets. Many drugs with a narrow absorption window that must be administered multiple times per day could potentially be developed into longer-lasting effective therapies that offer reduced daily administrations, greater patient compliance, reduced maximum plasma–related adverse effects, and improved intersubject variability. These novel dosage forms may create added value from the existing therapeutic franchise through the classic marketing strategies of product proliferation. And, finally, at a time when many drug companies are facing expiration of key patents, new oral bioadhesive formulations with improved performance can provide patent life extension and facilitate product life cycle management.

Although further research is required, orally administered pharmaceuticals of the future are likely to include bioadhesive microparticles and nanoparticles that will provide site-specific uptake of drugs and allow tailored drug release to meet biological needs. With the recent development in nanotechnology, bioadhesive nanodevices offer yet another tool to further expand the benefits. With the growing realization of the importance of nonspherical-shape particles, the functional behavior of these bioadhesive carriers can be tuned to optimize their performance in humans (64).

Acknowledgment

The author would like to thank Dr. George Grandolfi and Aliceann Hagopian for their valuable input.

Avinash Nangia, PhD, is senior vice-president of research and development at Spherics, Inc., 375 Forbes Blvd., Mansfield, MA 02048, tel. 508.452.7000, fax 508.452.7070,
.




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References

1. J.W. Lee, J.H. Park, and J.R. Robinson, "Bioadhesive-Based Dosage Forms: The Next Generation," J. Pharm. Sci. 89, 850–866 (2000).

2. M.A. Longer, H.S. Ch'ng, and J.R. Robinson, "Bioadhesive Polymers as Platforms for the Oral Controlled Drug Delivery III. Oral Delivery of Chlorthiazide using a Bioadhesive Polymer," J. Pharm. Sci. 70, 406–411 (1985).

3. M.R. Jimenez-Castellanos, H. Zia, and C.T. Rhodes, "Mucoadhesive Drug Delivery Systems," Drug Dev. Ind. Pharm. 19, 143–194 (1993).

4. H.E. Junginger, "Bioadhesive Polymer Systems for Peptide Delivery," Acta Pharm. Technol. 36, 110–126 (1990).

5. J. Woodley, "Bioadhesion: New Possibilities for Drug Administration?" Clin. Pharmacokinet. 40, 77–84 (2001).


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