Formulation and evaluation of insulin dry powder for pulmonary delivery

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

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Oral delivery is the most convenient and the most acceptable route. However, insulin by itself is degraded by intestinal enzymes and is not absorbed intact across the gastrointestinal mucosa. Now, a day gelatin, trypsin coated capsule, pill, pellets may be available. It has some disadvantages; a lot of the insulin will be wasted before it gets where it's going. Insulin taken as a pill is quickly broken down in the stomach, just like the food you eat. That makes it useless for lowering blood glucose levels. Intensified insulin therapy consists of basal insulin given in the form of either twice-daily injections of delayed action - lente or isoplane (NPH) insulin or once- or twice- daily injections of longer acting ultralente Continuous subcutaneous Insulin infusion (CSII) from a portal pump is used for basal insulin. Prandial insulin is given by injection of short-acting insulin given 30 min before meal. E.g. Insulin syringe, pen, an insulin pump. 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).
Original languageEnglish
Pages (from-to)1182-1189
Number of pages8
JournalInternational Journal of PharmTech Research
Volume1
Issue number4
Publication statusPublished - 2009

Fingerprint

Powders
Insulin
Lung
Injections
Meals
Short-Acting Insulin
Isophane Insulin
Mucociliary Clearance
Subcutaneous Infusions
Syringes
Gelatin
Trypsin
Capsules
Blood Glucose
Permeability
Stomach
Mucous Membrane
Epithelium
Food
Enzymes

Cite this

Shivanand, P., Amruta, C., Binal, P., Mahalaxmi, R., Viral, D., & Jivani, N. P. (2009). Formulation and evaluation of insulin dry powder for pulmonary delivery. International Journal of PharmTech Research, 1(4), 1182-1189.
Shivanand, P. ; Amruta, C. ; Binal, P. ; Mahalaxmi, R. ; Viral, D. ; Jivani, N.P. / Formulation and evaluation of insulin dry powder for pulmonary delivery. In: International Journal of PharmTech Research. 2009 ; Vol. 1, No. 4. pp. 1182-1189.
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title = "Formulation and evaluation of insulin dry powder for pulmonary delivery",
abstract = "Oral delivery is the most convenient and the most acceptable route. However, insulin by itself is degraded by intestinal enzymes and is not absorbed intact across the gastrointestinal mucosa. Now, a day gelatin, trypsin coated capsule, pill, pellets may be available. It has some disadvantages; a lot of the insulin will be wasted before it gets where it's going. Insulin taken as a pill is quickly broken down in the stomach, just like the food you eat. That makes it useless for lowering blood glucose levels. Intensified insulin therapy consists of basal insulin given in the form of either twice-daily injections of delayed action - lente or isoplane (NPH) insulin or once- or twice- daily injections of longer acting ultralente Continuous subcutaneous Insulin infusion (CSII) from a portal pump is used for basal insulin. Prandial insulin is given by injection of short-acting insulin given 30 min before meal. E.g. Insulin syringe, pen, an insulin pump. 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).",
author = "P. Shivanand and C. Amruta and P. Binal and R. Mahalaxmi and D. Viral and N.P. Jivani",
note = "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: insulin, 9004-10-8 Tradenames: aerodose, Aerogen; aerx idms, Aradigm; aerx idms, Novo Nordisk; exubera, Aventis; exubera, Nektar; exubera, Pfizer; promaxx, Alkermes; promaxx, Epic Therapeutics; promaxx, Lilly; spiros, Dura; spiros, Lilly; technosphere insulin system, MannKindJethaler; TransJector Manufacturers: Aerogen; Alkermes; Aradigm; Aventis; Dura; Epic Therapeutics; Lilly; MannKind; Nektar; Novo Nordisk; Pfizer References: 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; Labrude, P., Rasolomanana, M., Vigneron, C., Thirion, C., Chaillot, B., Protective effect of sucrose on Spray drying of ox hemoglobin (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; Binder, C., Lauritzen, T., Faber, O., Pramming, S., Insulin pharmacokinetics (1984) Diabetes Care, 7, pp. 188-199; 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; Dapergolas, G., Gregoriadis, G., Hypoglycemic effect of liposome entrapped insulin administered intragastrically into rats (1976) Lancet, pp. 824-827; 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; Lai, M.C., Topp, E.M., Solid-state chemical stability of proteins and peptides (1999) Journal of Pharmaceutical Sciences, 88 (5), pp. 489-500. , DOI 10.1021/js980374e; Miller, C.D., Phillips, L.S., Ziemer, D.C., Gallina, D.L., Cook, C.B., El-Kebbi, I.M., Hypoglycemia in patients with type 2 diabetes mellitus (2001) Archives of Internal Medicine, 161 (13), pp. 1653-1659; Freemantle, N., Blonde, L., Duhot, D., Availability of Inhaled Insulin Promotes Greater Perceived Acceptance of Insulin Therapy in Patients with Type 2 Diabetes; 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; Hayes, R.P., Muchmore, D.B., Stump, T.E., Silverman, B., Patient reported outcomes (PROs) using the Lilly/Alkermes inhaled insulin system versus injects able insulin in patients with type 1 diabetes (T1D) (2005) Diabetes, 54, pp. A495; www.emedicine.com/med/TOPIC543.HTM-83k; Goyal, R.K., Elements of Pharmacology, , Seventh edition. B.S. Shah Prakashan.Page no: 172; Dailey, G., A timely transition to insulin: Identifying type 2 diabetes patients failing oral therapy (2005) Formulary, 40 (4), pp. 114-130",
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Shivanand, P, Amruta, C, Binal, P, Mahalaxmi, R, Viral, D & Jivani, NP 2009, 'Formulation and evaluation of insulin dry powder for pulmonary delivery', International Journal of PharmTech Research, vol. 1, no. 4, pp. 1182-1189.

Formulation and evaluation of insulin dry powder for pulmonary delivery. / 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. 1182-1189.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Formulation and evaluation of insulin dry powder for pulmonary delivery

AU - Shivanand, P.

AU - Amruta, C.

AU - Binal, P.

AU - Mahalaxmi, R.

AU - Viral, D.

AU - Jivani, N.P.

N1 - 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: insulin, 9004-10-8 Tradenames: aerodose, Aerogen; aerx idms, Aradigm; aerx idms, Novo Nordisk; exubera, Aventis; exubera, Nektar; exubera, Pfizer; promaxx, Alkermes; promaxx, Epic Therapeutics; promaxx, Lilly; spiros, Dura; spiros, Lilly; technosphere insulin system, MannKindJethaler; TransJector Manufacturers: Aerogen; Alkermes; Aradigm; Aventis; Dura; Epic Therapeutics; Lilly; MannKind; Nektar; Novo Nordisk; Pfizer References: 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; Labrude, P., Rasolomanana, M., Vigneron, C., Thirion, C., Chaillot, B., Protective effect of sucrose on Spray drying of ox hemoglobin (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; Binder, C., Lauritzen, T., Faber, O., Pramming, S., Insulin pharmacokinetics (1984) Diabetes Care, 7, pp. 188-199; 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; Dapergolas, G., Gregoriadis, G., Hypoglycemic effect of liposome entrapped insulin administered intragastrically into rats (1976) Lancet, pp. 824-827; 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; Lai, M.C., Topp, E.M., Solid-state chemical stability of proteins and peptides (1999) Journal of Pharmaceutical Sciences, 88 (5), pp. 489-500. , DOI 10.1021/js980374e; Miller, C.D., Phillips, L.S., Ziemer, D.C., Gallina, D.L., Cook, C.B., El-Kebbi, I.M., Hypoglycemia in patients with type 2 diabetes mellitus (2001) Archives of Internal Medicine, 161 (13), pp. 1653-1659; Freemantle, N., Blonde, L., Duhot, D., Availability of Inhaled Insulin Promotes Greater Perceived Acceptance of Insulin Therapy in Patients with Type 2 Diabetes; 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; Hayes, R.P., Muchmore, D.B., Stump, T.E., Silverman, B., Patient reported outcomes (PROs) using the Lilly/Alkermes inhaled insulin system versus injects able insulin in patients with type 1 diabetes (T1D) (2005) Diabetes, 54, pp. A495; www.emedicine.com/med/TOPIC543.HTM-83k; Goyal, R.K., Elements of Pharmacology, , Seventh edition. B.S. Shah Prakashan.Page no: 172; Dailey, G., A timely transition to insulin: Identifying type 2 diabetes patients failing oral therapy (2005) Formulary, 40 (4), pp. 114-130

PY - 2009

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AB - Oral delivery is the most convenient and the most acceptable route. However, insulin by itself is degraded by intestinal enzymes and is not absorbed intact across the gastrointestinal mucosa. Now, a day gelatin, trypsin coated capsule, pill, pellets may be available. It has some disadvantages; a lot of the insulin will be wasted before it gets where it's going. Insulin taken as a pill is quickly broken down in the stomach, just like the food you eat. That makes it useless for lowering blood glucose levels. Intensified insulin therapy consists of basal insulin given in the form of either twice-daily injections of delayed action - lente or isoplane (NPH) insulin or once- or twice- daily injections of longer acting ultralente Continuous subcutaneous Insulin infusion (CSII) from a portal pump is used for basal insulin. Prandial insulin is given by injection of short-acting insulin given 30 min before meal. E.g. Insulin syringe, pen, an insulin pump. 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).

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VL - 1

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JO - International Journal of PharmTech Research

JF - International Journal of PharmTech Research

SN - 0974-4304

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