Nasal drug delivery bioadhesives

Ilium, L., Jorgensen, H., Bisgaard, H., Krogsgaard, O., and Rossing, N., Bioadhesive microspheres as a potential nasal drug delivery system, Int. J. Pharm., 39 189-199 (1987). 

Ilium, L., Bioadhesive Formulations for Nasal Peptide Delivery. In Bioadhesive Drug Delivery Systems (E. Mathiowitz, D.E. Chiekering, III, and C.-M. Lehr, eds.), Marcel Dekker, Inc., New York, 1999, pp. 507-539. 

A host of bioadhesive controlled release systems have been proposed in recent years. Among the most commonly studied applications of bioadhesive materials is the area of buccal controlled delivery [408], The buccal delivery of small peptides from bioadhesive polymers was studied by Bodde and coworkers [409], and a wide range of compositions based on poly(butyl acrylate) and/or poly(acrylic acid) gave satisfactory performance. Bioadhesive poly(acrylic add)-based formulations have also been used for oral applications [402,410] for the sustained delivery of chlorothiazide [410] and for a thin bioadhesive patch for treatment of gingivitis and periodontal disease [411]. Other bioadhesive applications of polyelectrolytes include materials for ophthalmic vehicles [412,413], and systems for oral [410,414,415-419], rectal [420,421] vaginal [422] and nasal [423] drug delivery. 

Bioadhesive formulations and microsphere delivery systems in particular have attracted much attention. As drug formulations are usually rapidly removed from the site of deposition by the mucociliary clearance, increasing the retention time of drug in the nasal cavity via bioadhesion can increase bioavailability [28], Bioadhesion may be defined as the ability of a material (synthetic or biological) to adhere to a biological tissue for an extended period of time. When applied to a mucous membrane, a bioadhesive polymer may adhere primarily to the mucus layer or epithelial cell surface in a phenomenon known as mucoadhesion [29,30]. The bioadhesive properties of a wide range of materials have been evaluated over the last decade. 

Nagai, T., and Y. Machida. 1990. Bioadhesive dosage forms for nasal administration, in Bioadhesive drug delivery systems, eds. V. Lenearts, and R. Gurny, 169. Florida CRC Press, chap. 9. 

Carbopol resins also have been used in controlled-release dosage forms. Especially, the resins Noven AA-1 USP and Carbopol 934P NF are being extensively developed in bioadhesive drug delivery systems for topical, bucal or nasal, ocular, and rectal applications (e.g., Fentanyl ). Noven CA-1 USP and CA-2 USP are used as oral laxative and antidiarrheal products in swallowable and chewable tablets. 

Ilium, L. (1999), Bioadhesive formulations for nasal peptide delivery, in Mathiowitz, E., Chickering, D. E., and Lehr, C.-M., Eds., Bioadhesive Drug Delivery Systems, Fundamentals, Novel Approaches and Development, Marcel Dekker, New York, pp. 507-539. 

Research on nasal powder drug delivery has employed polymers such as starch, dextrans, polyacrylic acid derivatives (e.g., carbopol, polycarbophil), cellulose derivatives (microcrystalline cellulose, semicrystalline cellulose, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, carboxymethyl cellulose), chitosan, sodium alginate, hyaluronans, and polyanhydrides such as poly(methyl vinyl ether-co-maleic anhydride) (PVM/MA). Many of these polymers have already been used as excipients in pharmaceutical formulations and are often referred to as first-generation bioadhesives [38-45], In nasal dry powder a single bioadhesive polymer or a... 

Dry powder formulations for nasal delivery of peptides and proteins have been investigated for the first time by Nagai and others [38], Since then, much research work has been done on dry powders containing bioadhesive polymers for nasal drug administration. The bioavailability and duration of action of drugs administered by the nasal route are increased by the use of the principle of mucoadhesion and dry powder formulations. Research work on dry powder formulation containing bioadhesive polymers is summarized in Table 1. 

Starch 1. Slow release drug delivery system based on amylose-rich starch has been marketed under the trade name Contramid . 2. Starch microspheres have been investigated as a bioadhesive drug delivery system for the nasal delivery of proteins. Khanlari and Dube (2013), Nair and Laurencin (2006), and Marques et al. (2002)... 

Mucoadhesive drug delivery systems are comprised of administration of drug across the mucosal membrane using a mucoadhesive/bioadhesive polymer through various noninvasive routes such as peroral, ocular, buccal, nasal, stomach, intestinal, colon, vaginal, rectal, cervical or vulval. The drug delivery systems, which have made use of chitosan as a carrier for administration through various routes, have been represented in Table 2.2. 

The nonperoral mucosal delivery routes such as buccal, nasal, and vaginal sites offer barriers to drug molecules similar to that of the peroral route. Drugs delivered via these routes have to be small (<300 Da), lipophilic in nature, and with low dosage regimen requirements. The different approaches used to deliver drugs across these mucosae include the use of enzyme inhibitors, penetration enhancers, bioadhesive patches, prodrugs, liposomes, and solubility modifiers.96,106,130... 

Varshosaz, J., Sadrai, H., and Heidari, A. (2006), Nasal delivery of insulin using bioadhesive chitosan gels, Drug Deliv., 13, 31-38. 

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