Application of hydrogel polymers for development of thyrotropin releasing hormone-loaded adhesive buccal patches

To utilize hydrogels for fabricating thyrotropin releasing hormone (TRH) adhesive buccal patches, type of hydrogels such as polyacrylic acids (Polycarbophil AA1, Carbopols 934P, 974P and 971P), celluloses (HPMC K4M, K4MCR and K15M), polysaccharide (sodium alginate) and polyacrylic acid combinations with either cellulose or polysaccharide were evaluated for adhesion force, water uptake and swelling capacity. Upon the characterization of hydrogel polymers, TRH-loading of patches fabricated from these hydrogels was evaluated at various polymer concentrations, combinations and ratios and then in vitro release kinetics of TRH from these patches were studied. Results indicated that maximum adhesion force was shown by polyacrylic acids. Adhesive force of polymer combination mainly resulted from combination of adhesive force, according to ratio proportion used, of each polymer without any superimposed effect of polymer combination. Polycarbophil AA1 showed highest water uptake and swelling capacity. Maximum TRH-loading was obtained with sodium alginate and Polycarbophil AA1 and sodium alginate combination. TRH release profiles revealed that release was sustained from Polycarbophil AA1 and its combination with celluloses or polysaccharide at 2:1 level of polymer ratio. Based on adhesion, loading and release characteristics, patches of Polycarbophil AA1 with K4M, K4MCR and sodium alginate were concluded to be suitable for further development.

[1]  F. A. Mohammed,et al.  Preparation and In Vitro/In Vivo Evaluation of the Buccal Bioadhesive Properties of Slow-Release Tablets Containing Miconazole Nitrate , 2003, Drug development and industrial pharmacy.

[2]  B. D. Rohera,et al.  Comparative evaluation of rate of hydration and matrix erosion of HEC and HPC and study of drug release from their matrices. , 2002, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[3]  X Huang,et al.  On the importance and mechanisms of burst release in matrix-controlled drug delivery systems. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[4]  N A Peppas,et al.  Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). , 2001, Advanced drug delivery reviews.

[5]  J. Robinson,et al.  Bioadhesive-based dosage forms: the next generation. , 2000, Journal of pharmaceutical sciences.

[6]  Manisha Chawla,et al.  Potential Applications of Carbomer in Oral Mucoadhesive Controlled Drug Delivery System: A Review , 2000, Drug development and industrial pharmacy.

[7]  Claus-Michael Lehr,et al.  Bioadhesive Drug Delivery Systems : Fundamentals, Novel Approaches, and Development , 1999 .

[8]  L. Nielsen,et al.  Bioadhesive drug delivery systems: I. Characterisation of mucoadhesive properties of systems based on glyceryl mono-oleate and glyceryl monolinoleate , 1998 .

[9]  Wayne R. Gombotz,et al.  Protein release from alginate matrices. , 1998, Advanced drug delivery reviews.

[10]  Shian-Min Wu,et al.  Stability of peptides during iontophoretic transdermal delivery , 1996 .

[11]  T. Nagai,et al.  Buccal delivery systems using hydrogels , 1993 .

[12]  Teruo Okano,et al.  Hydrogels: Swelling, Drug Loading, and Release , 1992, Pharmaceutical Research.

[13]  Y. Kiso,et al.  Lipophilic Peptides: Synthesis of Lauroyl Thyrotropin-Releasing Hormone and Its Biological Activity , 1991, Pharmaceutical Research.

[14]  Toguchi Hajime,et al.  Effects of counteranion of TRH and loading amount on control of TRH release from copoly(dl-lactic/glycolic acid) microspheres prepared by an in-water drying method , 1991 .

[15]  H. Merkle,et al.  Evaluation of laminated muco-adhesive patches for buccal drug delivery , 1989 .

[16]  G. Menon,et al.  High-Performance Liquid Chromatographic Assay for Thyrotropin Releasing Hormone and Benzyl Alcohol in Injectable Formulation , 1987, Pharmaceutical Research.

[17]  R. Burnette,et al.  Comparison between the iontophoretic and passive transport of thyrotropin releasing hormone across excised nude mouse skin. , 1986, Journal of pharmaceutical sciences.

[18]  N. Peppas,et al.  Bioadhesive intraoral release systems: design, testing and analysis. , 1984, Biomaterials.

[19]  J D Smart,et al.  An in‐vitro investigation of mucosa‐adhesive materials for use in controlled drug delivery , 1984, The Journal of pharmacy and pharmacology.

[20]  P. C. Hiemenz.  Polymer Chemistry: The Basic Concepts , 1984 .

[21]  H. Merkle,et al.  Buccal absorption of protirelin: an effective way to stimulate thyrotropin and prolactin. , 1983, Journal of pharmaceutical sciences.

[22]  Arvind Panwar.  Hypothalamic and pituitary hormones , 2010 .

[23]  J. Smart.  Recent developments in the use of bioadhesive systems for delivery of drugs to the oral cavity. , 2004, Critical reviews in therapeutic drug carrier systems.

[24]  Jie Zhang,et al.  Oral Mucosal Drug Delivery , 2002, Clinical pharmacokinetics.

[25]  P. P. Bhatt,et al.  Transmucosal delivery of oxytocin to rabbits using a mucoadhesive buccal patch. , 1997, Pharmaceutical development and technology.

[26]  P. P. Bhatt,et al.  Absorption of Thyrotropin-Releasing Hormone in Rats Using a Mucoadhesive Buccal Patch , 1997 .

[27]  I. Kellaway,et al.  MUCOADHESIVE HYDROGELS FOR BUCCAL DELIVERV , 1996 .

[28]  S. Yen,et al.  The enhanced iontophoretic transport of TRH and its impedance study , 1996 .

[29]  J. Reynolds.  Martindale : the extra pharmacopoeia , 1993 .

[30]  R. Gurny.  Bioadhesive Intraoral Release Systems , 1986 .

[31]  James L. Chen,et al.  CHAPTER 10 – COMPOSITIONS PRODUCING ADHESION THROUGH HYDRATION , 1970 .

[32]  R. M. Barrer,et al.  The diffusion and solution of gases in highly crosslinked copolymers , 1968 .

[33]  S. S. Voi︠u︡t︠s︡kiĭ.  Autohesion and adhesion of high polymers , 1963 .