Pulmonary delivery as a route for insulin

P. Shivanand, C. Amruta, P. Binal, R. Mahalaxmi, D. Viral, N.P. Jivani

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The pulmonary route of administration offers several advantages. First, the lung has a large surface area for drug absorption, ranging from 100 to 140 m2. In addition, the alveolar epithelium has permeability that allows for rapid absorption of solutes. Because the mucociliary clearance of the alveolar lung tissue is slower than that of the bronchiolar tissues, the alveoli provide a greater opportunity for the absorption of larger molecules (e.g., insulin). Studies have shown that particle size should be between 1 and 3 micrometers in diameter for optimal deposition in the lung, and that dry powder formulation can deliver more active drug in a single inhalation than liquid aerosol formulations. Patient-controlled variables (e.g., inhalation flow rate, inhaled volume, and duration of inhalation) also need to be controlled for optimal deep-lung insulin delivery. The pharmacodynamic effects of insulin formulations administered via the lung are comparable to, or even faster than, those of subcutaneous injected regular insulin or rapid-acting insulin analogues.
Original languageEnglish
Pages (from-to)1190-1197
Number of pages8
JournalInternational Journal of PharmTech Research
Volume1
Issue number4
Publication statusPublished - 2009

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Insulin
Lung
Inhalation
Short-Acting Insulin
Mucociliary Clearance
Aerosols
Particle Size
Pharmaceutical Preparations
Powders
Permeability
Epithelium

Cite this

Shivanand, P., Amruta, C., Binal, P., Mahalaxmi, R., Viral, D., & Jivani, N. P. (2009). Pulmonary delivery as a route for insulin. International Journal of PharmTech Research, 1(4), 1190-1197.
Shivanand, P. ; Amruta, C. ; Binal, P. ; Mahalaxmi, R. ; Viral, D. ; Jivani, N.P. / Pulmonary delivery as a route for insulin. In: International Journal of PharmTech Research. 2009 ; Vol. 1, No. 4. pp. 1190-1197.
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abstract = "The pulmonary route of administration offers several advantages. First, the lung has a large surface area for drug absorption, ranging from 100 to 140 m2. In addition, the alveolar epithelium has permeability that allows for rapid absorption of solutes. Because the mucociliary clearance of the alveolar lung tissue is slower than that of the bronchiolar tissues, the alveoli provide a greater opportunity for the absorption of larger molecules (e.g., insulin). Studies have shown that particle size should be between 1 and 3 micrometers in diameter for optimal deposition in the lung, and that dry powder formulation can deliver more active drug in a single inhalation than liquid aerosol formulations. Patient-controlled variables (e.g., inhalation flow rate, inhaled volume, and duration of inhalation) also need to be controlled for optimal deep-lung insulin delivery. The pharmacodynamic effects of insulin formulations administered via the lung are comparable to, or even faster than, those of subcutaneous injected regular insulin or rapid-acting insulin analogues.",
author = "P. Shivanand and C. Amruta and P. Binal and R. Mahalaxmi and D. Viral and N.P. Jivani",
note = "Cited By :3 Export Date: 10 November 2017 Correspondence Address: Shivanand, P.; Smt. R. B. P. M. Pharmacy College, Atkot-360040, Rajkot, Gujarat, India; email: dot.shivanand@gmail.com Chemicals/CAS: citric acid, 126-44-3, 5949-29-1, 77-92-9, 8002-14-0; insulin, 9004-10-8; insulin lispro, 133107-64-9; mannitol, 69-65-8, 87-78-5; protein tyrosine kinase, 80449-02-1 Tradenames: aerx idms; exubera, Nektar Manufacturers: Nektar References: Costantino, H.R., Moisture induced Aggregation of Lyophilized Insulin (1994) Pharm Res., 11, pp. 21-29; Izutsu, K., Yoshika, S., Terao, T., Effect on mannitol crystallinity on the stabilization of enzymes during freeze-drying (1994) Chem. Pharm. Bull., 42, pp. 5-8. , Tokyo; Kobayasi, S., Kondo, S., Juni, K., Study on Pulmonary delivary of salmon calcitonin in rats: Effect of protease inhibitors and absorption enhancers (1994) Pharm. Res., 11, pp. 1239-1243; Labrude, P., Rasolomanana, M., Vigneron, C., Thirion, C., Chaillot, B., Protective effect of sucrose on Spray drying of oxyhemoglobin (1989) J., Pharm. Sci., 78, pp. 223-229; Maa, Y.F., Nguyen, P.A., Andya, J.D., Dasovich, N., Sweeney, T.D., Shire, S.J., Hsu, C.C., (1998) Effect of Spray Drying, 87, pp. 1406-1411; Schade, D.S., Eaton, R.P., Insulin delivery: How, when, where (1985) N Engl J Med, 312, pp. 1120-1121; Pierce, A.E., Risdall, P.C., Shaw, B., Absorption of orally Administered insulin by the newly born Calf (1964) J 'Physiol, 171, pp. 203-215; Laube, B.L., Georgopoulos, A., Adams III, G.K., Preliminary study of the efficacy of insulin aerosol delivered by oral inhalation in diabetic patients (1993) Journal of the American Medical Association, 269 (16), pp. 2106-2109. , DOI 10.1001/jama.269.16.2106; Saydah, S.H., Fradkin, J., Cowie, C.C., Poor Control of Risk Factors for Vascular Disease among Adults with Previously Diagnosed Diabetes (2004) Journal of the American Medical Association, 291 (3), pp. 335-342. , DOI 10.1001/jama.291.3.335; Polonsky, W.H., Fisher, L., Guzman, S., Villa-Caballero, L., Edelman, S.V., Psychological Insulin Resistance in Patients with Type 2 Diabetes: The Scope of the Problem; Dailey, G., A timely transition to insulin: Identifying type 2 diabetes patients failing oral therapy (2005) Formulary, 40 (4), pp. 114-130; Boss, A.H., Grant, M.L., Cheatham, W.W., Mimicry of the early phase insulin response in humans with rapidly available inhaled insulin accelerates postprandial glucose disposal compared to slower bioavailable insulin (2005) Diabetes, 54, pp. A333; Rosenstock, J., Cappelleri, J.C., Bolinder, B., Gerber, R.A., Patient Satisfaction and Glycemic Control after 1 Year with Inhaled Insulin (Exubera) in Patients with Type 1 or Type 2 Diabetes; Fineberg, S.E., Kawabata, T., Finco-Kent, D., Liu, C., Krasner, A., Antibody response to inhaled insulin in patients with type 1 or type 2 diabetes. An analysis of initial phase II and III inhaled insulin (Exubera) trials and a two-year extension trial (2005) Journal of Clinical Endocrinology and Metabolism, 90 (6), pp. 3287-3294. , http://jcem.endojournals.org/cgi/reprint/90/6/3295, DOI 10.1210/jc.2004-2229; Heise, T., Bott, S., Tusek, C., (1998) The Methods and Compositions for the Aerosolization and Systemic Delivery of Insulin to a Mammalian Host; Sha, S., Becker, R., Willavise, S., The effect of smoking cessation on absorption of inhaled insulin (Exubera) (2002) Diabetes, 51 (SUPPL. 1), pp. A133. , Abstract 538",
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Shivanand, P, Amruta, C, Binal, P, Mahalaxmi, R, Viral, D & Jivani, NP 2009, 'Pulmonary delivery as a route for insulin', International Journal of PharmTech Research, vol. 1, no. 4, pp. 1190-1197.

Pulmonary delivery as a route for insulin. / Shivanand, P.; Amruta, C.; Binal, P.; Mahalaxmi, R.; Viral, D.; Jivani, N.P.

In: International Journal of PharmTech Research, Vol. 1, No. 4, 2009, p. 1190-1197.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Pulmonary delivery as a route for insulin

AU - Shivanand, P.

AU - Amruta, C.

AU - Binal, P.

AU - Mahalaxmi, R.

AU - Viral, D.

AU - Jivani, N.P.

N1 - Cited By :3 Export Date: 10 November 2017 Correspondence Address: Shivanand, P.; Smt. R. B. P. M. Pharmacy College, Atkot-360040, Rajkot, Gujarat, India; email: dot.shivanand@gmail.com Chemicals/CAS: citric acid, 126-44-3, 5949-29-1, 77-92-9, 8002-14-0; insulin, 9004-10-8; insulin lispro, 133107-64-9; mannitol, 69-65-8, 87-78-5; protein tyrosine kinase, 80449-02-1 Tradenames: aerx idms; exubera, Nektar Manufacturers: Nektar References: Costantino, H.R., Moisture induced Aggregation of Lyophilized Insulin (1994) Pharm Res., 11, pp. 21-29; Izutsu, K., Yoshika, S., Terao, T., Effect on mannitol crystallinity on the stabilization of enzymes during freeze-drying (1994) Chem. Pharm. Bull., 42, pp. 5-8. , Tokyo; Kobayasi, S., Kondo, S., Juni, K., Study on Pulmonary delivary of salmon calcitonin in rats: Effect of protease inhibitors and absorption enhancers (1994) Pharm. Res., 11, pp. 1239-1243; Labrude, P., Rasolomanana, M., Vigneron, C., Thirion, C., Chaillot, B., Protective effect of sucrose on Spray drying of oxyhemoglobin (1989) J., Pharm. Sci., 78, pp. 223-229; Maa, Y.F., Nguyen, P.A., Andya, J.D., Dasovich, N., Sweeney, T.D., Shire, S.J., Hsu, C.C., (1998) Effect of Spray Drying, 87, pp. 1406-1411; Schade, D.S., Eaton, R.P., Insulin delivery: How, when, where (1985) N Engl J Med, 312, pp. 1120-1121; Pierce, A.E., Risdall, P.C., Shaw, B., Absorption of orally Administered insulin by the newly born Calf (1964) J 'Physiol, 171, pp. 203-215; Laube, B.L., Georgopoulos, A., Adams III, G.K., Preliminary study of the efficacy of insulin aerosol delivered by oral inhalation in diabetic patients (1993) Journal of the American Medical Association, 269 (16), pp. 2106-2109. , DOI 10.1001/jama.269.16.2106; Saydah, S.H., Fradkin, J., Cowie, C.C., Poor Control of Risk Factors for Vascular Disease among Adults with Previously Diagnosed Diabetes (2004) Journal of the American Medical Association, 291 (3), pp. 335-342. , DOI 10.1001/jama.291.3.335; Polonsky, W.H., Fisher, L., Guzman, S., Villa-Caballero, L., Edelman, S.V., Psychological Insulin Resistance in Patients with Type 2 Diabetes: The Scope of the Problem; Dailey, G., A timely transition to insulin: Identifying type 2 diabetes patients failing oral therapy (2005) Formulary, 40 (4), pp. 114-130; Boss, A.H., Grant, M.L., Cheatham, W.W., Mimicry of the early phase insulin response in humans with rapidly available inhaled insulin accelerates postprandial glucose disposal compared to slower bioavailable insulin (2005) Diabetes, 54, pp. A333; Rosenstock, J., Cappelleri, J.C., Bolinder, B., Gerber, R.A., Patient Satisfaction and Glycemic Control after 1 Year with Inhaled Insulin (Exubera) in Patients with Type 1 or Type 2 Diabetes; Fineberg, S.E., Kawabata, T., Finco-Kent, D., Liu, C., Krasner, A., Antibody response to inhaled insulin in patients with type 1 or type 2 diabetes. An analysis of initial phase II and III inhaled insulin (Exubera) trials and a two-year extension trial (2005) Journal of Clinical Endocrinology and Metabolism, 90 (6), pp. 3287-3294. , http://jcem.endojournals.org/cgi/reprint/90/6/3295, DOI 10.1210/jc.2004-2229; Heise, T., Bott, S., Tusek, C., (1998) The Methods and Compositions for the Aerosolization and Systemic Delivery of Insulin to a Mammalian Host; Sha, S., Becker, R., Willavise, S., The effect of smoking cessation on absorption of inhaled insulin (Exubera) (2002) Diabetes, 51 (SUPPL. 1), pp. A133. , Abstract 538

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AB - The pulmonary route of administration offers several advantages. First, the lung has a large surface area for drug absorption, ranging from 100 to 140 m2. In addition, the alveolar epithelium has permeability that allows for rapid absorption of solutes. Because the mucociliary clearance of the alveolar lung tissue is slower than that of the bronchiolar tissues, the alveoli provide a greater opportunity for the absorption of larger molecules (e.g., insulin). Studies have shown that particle size should be between 1 and 3 micrometers in diameter for optimal deposition in the lung, and that dry powder formulation can deliver more active drug in a single inhalation than liquid aerosol formulations. Patient-controlled variables (e.g., inhalation flow rate, inhaled volume, and duration of inhalation) also need to be controlled for optimal deep-lung insulin delivery. The pharmacodynamic effects of insulin formulations administered via the lung are comparable to, or even faster than, those of subcutaneous injected regular insulin or rapid-acting insulin analogues.

M3 - Article

VL - 1

SP - 1190

EP - 1197

JO - International Journal of PharmTech Research

JF - International Journal of PharmTech Research

SN - 0974-4304

IS - 4

ER -

Shivanand P, Amruta C, Binal P, Mahalaxmi R, Viral D, Jivani NP. Pulmonary delivery as a route for insulin. International Journal of PharmTech Research. 2009;1(4):1190-1197.