Year : 2012 | Volume
: 4 | Issue : 2 | Page : 95-
Systemic delivery of biopharmaceuticals: Parenteral forever?
Assistant Professor in Pharmaceutics, IBB-Institute for Biotechnology and Bioengineering, Centre for Molecular and Structural Biomedicine, Faculty of Sciences and Technology - University of Algarve, Campus Gambelas, Building 8, Room 2.4, Lab 2.22, 8005-139 Faro, Portugal
Assistant Professor in Pharmaceutics, IBB-Institute for Biotechnology and Bioengineering, Centre for Molecular and Structural Biomedicine, Faculty of Sciences and Technology - University of Algarve, Campus Gambelas, Building 8, Room 2.4, Lab 2.22, 8005-139 Faro
|How to cite this article:|
Grenha A. Systemic delivery of biopharmaceuticals: Parenteral forever?.J Pharm Bioall Sci 2012;4:95-95
|How to cite this URL:|
Grenha A. Systemic delivery of biopharmaceuticals: Parenteral forever?. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Sep 20 ];4:95-95
Available from: http://www.jpbsonline.org/text.asp?2012/4/2/95/94807
The subject of systemic delivery of biopharmaceuticals has been discussed on some occasions in the Journal of Pharmacy and Bioallied Sciences, which is now in its eleventh issue. The last decades have witnessed a strong biotechnological progress, making available many biopharmaceuticals with great therapeutic potential, in many cases promising an undisputed place alongside other established therapies. The meaning of biopharmaceuticals is sometimes misleading, but strictly, this word refers to therapeutic molecules that are biological in nature and manufactured using biotechnology. In this sense, a considerably wide variety of macromolecules is included in this group, from proteins and peptides to antigens and nucleic acids. Their administration is extremely challenging because of biopharmaceutical and physicochemical limitations, requiring circumventing enzymatic degradation and reducing immune reactions, while ensuring molecular stability and permeability. Parenteral administration appears in this context as an obvious option, as it overcomes some of the referred issues. Actually, to date, a vast majority of marketed biopharmaceuticals is administered by direct injection, usually through the intravenous, subcutaneous or intramuscular route. However, the associated cost and patient discomfort have turned the research efforts of both the industrial and academic partners toward alternative possibilities that increase patient compliance.
The compelling need to address the issues mentioned herewith, has prompted the design of a number of strategies that permit needle-free administration, conjugating the identification of alternative routes of administration with the necessary development of adequate drug delivery carriers. Mucosal routes have thus been proposed to replace parenteral routes, as mucosal administration might be envisaged to provide a non-invasive systemic pathway. Oral, buccal, nasal, pulmonary, transdermal, and vaginal routes are all accepted for systemic biopharmaceutical delivery. However, poor patient acceptability of certain routes like the vaginal, reserves their use for local effect only. Nevertheless, the oral, nasal, pulmonary, and transdermal routes are taking the forefront of alternative drug delivery, with some technologies already available commercially. The Biphasix TM technology (Helix BioPharma) addresses transdermal delivery using liposomes, as do the ImuXen® technology (Lipoxen) for oral delivery of DNA and vaccines, and the AERx® technology (Aradigm Corporation) for pulmonary delivery. Still in pulmonary delivery, the Technosphere® technology (Mannkind Corporation) comprises of insulin-loaded dry powder microspheres, which are in phase III clinical trials. Importantly, a dry powder formulation of insulin (Exubera® ) was previously marketed by Pfizer, but was withdrawn from market by the company, allegedly because of reduced patient adherence to the novel therapeutic strategy. As can be seen, mucosal administration of biopharmaceuticals is inseparable from the task of designing suitable drug carriers. In this sense, as it was stated in a previous Editorial of this journal (Vol. 2, Issue 2, 2010), in many cases, nanomedicines seem to have taken advantage, with many reports providing the possibility of making stable effective drugs from unstable biopharmaceuticals. In any case, the carrier is required to maintain the native structure and the biological activity of the encapsulated biopharmaceutical during preparation, delivery, and storage.
With such technologies already in the market, and so many others being developed worldwide by academic and industrial researchers, it seems justified to state that the future of biopharmaceutical administration will be progressively shifted from injectable preparations to more user-friendly formulations, with the striking advantage of the mucosal routes relying on their non-invasiveness.