Applying the taguchi method to optimize sumatriptan succinate niosomes as drug carriers for skin delivery
Niosomes formulated from different nonionic surfactants (Span® 60, Brij® 72, Span® 80, or Eumulgin® B 2) with cholesterol (CH) molar ratios of 3:1 or 4:1 with respect to surfactant were prepared with different sumatriptan amount (10 and 15 mg) and stearylamine (SA). Thin‐film hydration method was em...
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Published in | Journal of pharmaceutical sciences Vol. 101; no. 10; pp. 3845 - 3863 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
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Elsevier Inc
01.10.2012
Wiley Subscription Services, Inc., A Wiley Company Wiley American Pharmaceutical Association Elsevier Limited |
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Abstract | Niosomes formulated from different nonionic surfactants (Span® 60, Brij® 72, Span® 80, or Eumulgin® B 2) with cholesterol (CH) molar ratios of 3:1 or 4:1 with respect to surfactant were prepared with different sumatriptan amount (10 and 15 mg) and stearylamine (SA). Thin‐film hydration method was employed to produce the vesicles, and the time lapsed to hydrate the lipid film (1 or 24 h) was introduced as variable. These factors were selected as variables and their levels were introduced into two L18 orthogonal arrays. The aim was to optimize the manufacturing conditions by applying Taguchi methodology. Response variables were vesicle size, zeta potential (Z), and drug entrapment. From Taguchi analysis, drug concentration and the time until the hydration were the most influencing parameters on size, being the niosomes made with Span® 80 the smallest vesicles. The presence of SA into the vesicles had a relevant influence on Z values. All the factors except the surfactant–CH ratio had an influence on the encapsulation. Formulations were optimized by applying the marginal means methodology. Results obtained showed a good correlation between mean and signal‐to‐noise ratio parameters, indicating the feasibility of the robust methodology to optimize this formulation. Also, the extrusion process exerted a positive influence on the drug entrapment. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3845–3863, 2012 |
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AbstractList | Niosomes formulated from different nonionic surfactants (Span® 60, Brij® 72, Span® 80, or Eumulgin® B 2) with cholesterol (CH) molar ratios of 3:1 or 4:1 with respect to surfactant were prepared with different sumatriptan amount (10 and 15 mg) and stearylamine (SA). Thin‐film hydration method was employed to produce the vesicles, and the time lapsed to hydrate the lipid film (1 or 24 h) was introduced as variable. These factors were selected as variables and their levels were introduced into two L18 orthogonal arrays. The aim was to optimize the manufacturing conditions by applying Taguchi methodology. Response variables were vesicle size, zeta potential (Z), and drug entrapment. From Taguchi analysis, drug concentration and the time until the hydration were the most influencing parameters on size, being the niosomes made with Span® 80 the smallest vesicles. The presence of SA into the vesicles had a relevant influence on Z values. All the factors except the surfactant–CH ratio had an influence on the encapsulation. Formulations were optimized by applying the marginal means methodology. Results obtained showed a good correlation between mean and signal‐to‐noise ratio parameters, indicating the feasibility of the robust methodology to optimize this formulation. Also, the extrusion process exerted a positive influence on the drug entrapment. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3845–3863, 2012 Niosomes formulated from different nonionic surfactants (Span® 60, Brij® 72, Span® 80, or Eumulgin® B 2) with cholesterol (CH) molar ratios of 3:1 or 4:1 with respect to surfactant were prepared with different sumatriptan amount (10 and 15 mg) and stearylamine (SA). Thin-film hydration method was employed to produce the vesicles, and the time lapsed to hydrate the lipid film (1 or 24 h) was introduced as variable. These factors were selected as variables and their levels were introduced into two L18 orthogonal arrays. The aim was to optimize the manufacturing conditions by applying Taguchi methodology. Response variables were vesicle size, zeta potential (Z), and drug entrapment. From Taguchi analysis, drug concentration and the time until the hydration were the most influencing parameters on size, being the niosomes made with Span® 80 the smallest vesicles. The presence of SA into the vesicles had a relevant influence on Z values. All the factors except the surfactant-CH ratio had an influence on the encapsulation. Formulations were optimized by applying the marginal means methodology. Results obtained showed a good correlation between mean and signal-to-noise ratio parameters, indicating the feasibility of the robust methodology to optimize this formulation. Also, the extrusion process exerted a positive influence on the drug entrapment. Niosomes formulated from different nonionic surfactants (Span 60, Brij 72, Span 80, or Eumulgin B 2) with cholesterol (CH) molar ratios of 3:1 or 4:1 with respect to surfactant were prepared with different sumatriptan amount (10 and 15mg) and stearylamine (SA). Thin-film hydration method was employed to produce the vesicles, and the time lapsed to hydrate the lipid film (1 or 24h) was introduced as variable. These factors were selected as variables and their levels were introduced into two L18 orthogonal arrays. The aim was to optimize the manufacturing conditions by applying Taguchi methodology. Response variables were vesicle size, zeta potential (Z), and drug entrapment. From Taguchi analysis, drug concentration and the time until the hydration were the most influencing parameters on size, being the niosomes made with Span 80 the smallest vesicles. The presence of SA into the vesicles had a relevant influence on Z values. All the factors except the surfactant-CH ratio had an influence on the encapsulation. Formulations were optimized by applying the marginal means methodology. Results obtained showed a good correlation between mean and signal-to-noise ratio parameters, indicating the feasibility of the robust methodology to optimize this formulation. Also, the extrusion process exerted a positive influence on the drug entrapment. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3845-3863, 2012 [PUBLICATION ABSTRACT] |
Author | Villasmil, Sheila Mouram, Imane Rabasco, Antonio M. Cózar‐bernal, Ma Jose González‐rodríguez, Maria Luisa |
Author_xml | – sequence: 1 givenname: Maria Luisa surname: González‐rodríguez fullname: González‐rodríguez, Maria Luisa email: malugoro@us.es organization: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain – sequence: 2 givenname: Imane surname: Mouram fullname: Mouram, Imane organization: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain – sequence: 3 givenname: Ma Jose surname: Cózar‐bernal fullname: Cózar‐bernal, Ma Jose email: malugoro@us.es organization: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain – sequence: 4 givenname: Sheila surname: Villasmil fullname: Villasmil, Sheila organization: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain – sequence: 5 givenname: Antonio M. surname: Rabasco fullname: Rabasco, Antonio M. organization: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain |
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Keywords | surfactants liposomes cationic lipids transdermal drug delivery extrusion skin factorial design light scattering (dynamic) HPLC (high‐performance/pressure liquid chromatography) permeation enhancers Performance evaluation Agonist Sumatriptan HPLC chromatography Lipids Drug carrier 5-HT1 Serotonine receptor Serotonin agonist Surfactant Niosome HPLC (high-performance/pressure liquid chromatography) Percutaneous route Triptan derivatives Taguchi method Pharmaceutical technology Antimigrainous agent Light scattering Liposome Liquid chromatography High pressure Extrusion Cations Skin Absorption enhancer Performance Factorial design |
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SubjectTerms | Administration, Cutaneous Biological and medical sciences cationic lipids Chemistry, Pharmaceutical - methods Cholesterol - administration & dosage Cholesterol - chemistry Drug Carriers - administration & dosage Drug Carriers - chemistry Drug Delivery Systems - methods Drug Stability extrusion factorial design General pharmacology HPLC (high‐performance/pressure liquid chromatography) light scattering (dynamic) liposomes Liposomes - administration & dosage Liposomes - chemistry Medical sciences Particle Size permeation enhancers Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Signal-To-Noise Ratio skin Skin - metabolism Solubility Sumatriptan - administration & dosage Sumatriptan - chemistry Surface-Active Agents - administration & dosage Surface-Active Agents - chemistry surfactants transdermal drug delivery |
Title | Applying the taguchi method to optimize sumatriptan succinate niosomes as drug carriers for skin delivery |
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