Галерея 3465127

Галерея 3465127
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Int J Pharm Investig

v.1(2); Apr-Jun 2011

PMC3465127

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Int J Pharm Investig. 2011 Apr-Jun; 1(2): 112–118.
Department of Pharmaceutics, Atmiya Institute of Pharmacy, Kalawad Road, Rajkot, Gujarat, India .
1 Smt. R. D. Gardi B. Pharmacy College, Nyara, Rajkot, Gujarat, India .
2 Department of Pharmaceutical Sciences, Saurashtra University, Rajkot, Gujarat, India .
Address for correspondence: Mr. Jaydeep Patel, Atmiya Institute of Pharmacy, Kalawad Road, Rajkot - 360 005, Gujarat, India. E-mail: moc.liamg@7letapmj
Received 2011 Jan 11; Revised 2011 Feb 21; Accepted 2011 Mar 2.
Copyright : © International Journal of Pharmaceutical Investigation
This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Keywords: Bioavailability, poor water solubility, self-nanoemulsifying drug delivery system, telmisartan
1. Stegemann S, Leveiller F, Franchi D, de Jong H, Lindén H. When poor solubility becomes an issue: From early stage to proof of concept. Eur J Pharm Sci. 2007; 31 :249–61. [ PubMed ] [ Google Scholar ]
2. Hauss DJ. Oral lipid based formulations. Adv Drug Deliv Rev. 2007; 59 :667–76. [ PubMed ] [ Google Scholar ]
3. Pouton CW. Formulation of self-emulsifying drug delivery systems. Adv Drug Deliv Rev. 1997; 25 :47–58. [ Google Scholar ]
4. Pouton CW. Lipid formulations for oral administration of drugs: Non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems. Eur J Pharm Sci. 2000; 11 :S93–8. [ PubMed ] [ Google Scholar ]
5. Pouton CW. Formulation of poorly water-soluble drugs for oral administration: Physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci. 2006; 29 :278–87. [ PubMed ] [ Google Scholar ]
6. Date AA, Nagarsenker MS. Design and evaluation of self nanoemulsified drug delivery systems (SNEDDS) for Cefpodoxime Proxetil. Int J Pharm. 2007; 329 :166–72. [ PubMed ] [ Google Scholar ]
7. Azeem A, Rizwan M, Ahmad FJ, Iqbal Z, Khar RK, Aqil M, et al. Nanoemulsion components screening and selection: A technical note. AAPS PharmSciTech. 2009; 10 :69–76. [ PMC free article ] [ PubMed ] [ Google Scholar ]
8. Singh AK, Chaurasiya A, Singh M, Upadhyay SC, Mukherjee R, Khar RK. Exemestane Loaded Self-Microemulsifying drug delivery system (SMEDDS): Development and optimization. AAPS PharmSciTech. 2008; 9 :628–34. [ PMC free article ] [ PubMed ] [ Google Scholar ]
9. Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of self microemulsifying drug delivery system of oridonin. Int J Pharm. 2008; 355 :269–76. [ PubMed ] [ Google Scholar ]
10. Porter CJ, Pouton CW, Cuine JF, Charman WN. Enhancing intestinal drug solubilisation using lipid-based delivery systems. Adv Drug Deliv Rev. 2008; 60 :673–91. [ PubMed ] [ Google Scholar ]
11. Chen ML. Lipid excipients and delivery systems for pharmaceutical development: A regulatory perspective. Adv Drug Deliv Rev. 2008; 60 :768–77. [ PubMed ] [ Google Scholar ]
12. Constanitinides PP, Scalart JP, Lancaster C, Marcello J, Marks G, Ellens H, et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm Res. 1994; 11 :1385–90. [ PubMed ] [ Google Scholar ]
13. Gershanik T, Benzeno S, Benita S. Interaction of a self-emulsifying lipid drug delivery system with the everted rat intestinal mucosa as a function of droplet size and surface charge. Pharm Res. 1998; 15 :863–9. [ PubMed ] [ Google Scholar ]
14. Müller RH, Jacobs C, Kayser O. Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future. Adv Drug Deliv Rev. 2001; 47 :3–19. [ PubMed ] [ Google Scholar ]
15. Nazzal S, Smalyukh II, Lavrentovich OD, Khan MA. Preparation and in vitro characterization of a eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: Mechanism and progress of emulsion formation. Int J Pharm. 2002; 235 :247–65. [ PubMed ] [ Google Scholar ]
16. Gao ZG, Choi HG, Shin HJ, Park KM, Lim SJ, Hwang KJ, et al. Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosphorin A. Int J Pharm. 1998; 161 :75–86. [ Google Scholar ]
Articles from International Journal of Pharmaceutical Investigation are provided here courtesy of Wolters Kluwer -- Medknow Publications
1. Stegemann S, Leveiller F, Franchi D, de Jong H, Lindén H. When poor solubility becomes an issue: From early stage to proof of concept. Eur J Pharm Sci. 2007; 31 :249–61. [ PubMed ] [ Google Scholar ] [ Ref list ]
2. Hauss DJ. Oral lipid based formulations. Adv Drug Deliv Rev. 2007; 59 :667–76. [ PubMed ] [ Google Scholar ] [ Ref list ]
5. Pouton CW. Formulation of poorly water-soluble drugs for oral administration: Physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci. 2006; 29 :278–87. [ PubMed ] [ Google Scholar ] [ Ref list ]
6. Date AA, Nagarsenker MS. Design and evaluation of self nanoemulsified drug delivery systems (SNEDDS) for Cefpodoxime Proxetil. Int J Pharm. 2007; 329 :166–72. [ PubMed ] [ Google Scholar ] [ Ref list ]
7. Azeem A, Rizwan M, Ahmad FJ, Iqbal Z, Khar RK, Aqil M, et al. Nanoemulsion components screening and selection: A technical note. AAPS PharmSciTech. 2009; 10 :69–76. [ PMC free article ] [ PubMed ] [ Google Scholar ] [ Ref list ]
8. Singh AK, Chaurasiya A, Singh M, Upadhyay SC, Mukherjee R, Khar RK. Exemestane Loaded Self-Microemulsifying drug delivery system (SMEDDS): Development and optimization. AAPS PharmSciTech. 2008; 9 :628–34. [ PMC free article ] [ PubMed ] [ Google Scholar ] [ Ref list ]
9. Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of self microemulsifying drug delivery system of oridonin. Int J Pharm. 2008; 355 :269–76. [ PubMed ] [ Google Scholar ] [ Ref list ]
4. Pouton CW. Lipid formulations for oral administration of drugs: Non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems. Eur J Pharm Sci. 2000; 11 :S93–8. [ PubMed ] [ Google Scholar ] [ Ref list ]
10. Porter CJ, Pouton CW, Cuine JF, Charman WN. Enhancing intestinal drug solubilisation using lipid-based delivery systems. Adv Drug Deliv Rev. 2008; 60 :673–91. [ PubMed ] [ Google Scholar ] [ Ref list ]
11. Chen ML. Lipid excipients and delivery systems for pharmaceutical development: A regulatory perspective. Adv Drug Deliv Rev. 2008; 60 :768–77. [ PubMed ] [ Google Scholar ] [ Ref list ]
3. Pouton CW. Formulation of self-emulsifying drug delivery systems. Adv Drug Deliv Rev. 1997; 25 :47–58. [ Google Scholar ] [ Ref list ]
12. Constanitinides PP, Scalart JP, Lancaster C, Marcello J, Marks G, Ellens H, et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm Res. 1994; 11 :1385–90. [ PubMed ] [ Google Scholar ] [ Ref list ]
13. Gershanik T, Benzeno S, Benita S. Interaction of a self-emulsifying lipid drug delivery system with the everted rat intestinal mucosa as a function of droplet size and surface charge. Pharm Res. 1998; 15 :863–9. [ PubMed ] [ Google Scholar ] [ Ref list ]
14. Müller RH, Jacobs C, Kayser O. Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future. Adv Drug Deliv Rev. 2001; 47 :3–19. [ PubMed ] [ Google Scholar ] [ Ref list ]
15. Nazzal S, Smalyukh II, Lavrentovich OD, Khan MA. Preparation and in vitro characterization of a eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: Mechanism and progress of emulsion formation. Int J Pharm. 2002; 235 :247–65. [ PubMed ] [ Google Scholar ] [ Ref list ]
16. Gao ZG, Choi HG, Shin HJ, Park KM, Lim SJ, Hwang KJ, et al. Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosphorin A. Int J Pharm. 1998; 161 :75–86. [ Google Scholar ] [ Ref list ]

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Department of Pharmaceutics, Atmiya Institute of Pharmacy, Kalawad Road, Rajkot, Gujarat, India .
Department of Pharmaceutics, Atmiya Institute of Pharmacy, Kalawad Road, Rajkot, Gujarat, India .
1 Smt. R. D. Gardi B. Pharmacy College, Nyara, Rajkot, Gujarat, India .
2 Department of Pharmaceutical Sciences, Saurashtra University, Rajkot, Gujarat, India .
2 Department of Pharmaceutical Sciences, Saurashtra University, Rajkot, Gujarat, India .
Telmisartan (TEL) is an angiotensin II receptor blocker (ARB) antihypertensive agent. The aim of the present investigation was to develop a self-nanoemulsifying drug delivery system (SNEDDS) to enhance the oral bioavailability of poorly water soluble TEL.
The solubility of TEL in various oils was determined to identify the oil phase of a SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify the selected oil. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsifying region. A SNEDDS was further evaluated for its percentage transmittance, emulsification time, drug content, phase separation, dilution, droplet size, zeta potential, pH, refractive index, and viscosity.
The developed SNEDDS formulation contained TEL (20 mg), Tween ® 20 (43.33%w/w), Carbitol ® (21.67%w/w), and Acrysol ® EL 135 (32%w/w). The optimized formulation of the TEL-loaded SNEDDS exhibited a complete in vitro drug release in 15 min as compared with the plain drug, which had a limited dissolution rate. It was also compared with the pure drug suspension by oral administration in male Wister rats. The in vivo study exhibited a 7.5-fold increase in the oral bioavailability of TEL from the SNEDDS compared with the pure drug suspension.
These results suggest the potential use of the SNEDDS to improve the dissolution and oral bioavailability of poorly water soluble TEL.
Oral route is the easiest and most convenient way of noninvasive administration. However, the oral drug delivery may hamper drug molecules that exhibit poor aqueous solubility. Approximately, 40% of new chemical entities exhibit a poor aqueous solubility and present a major challenge to modern drug delivery systems which leads to a poor oral bioavailability, high intra- and intersubject variability, and lack of dose proportionality. These drugs are classified as class II drug by the Biopharmaceutical Classification System (BCS), drugs with a poor aqueous solubility and high permeability.[ 1 ] Different formulation approaches like micronization, solid dispersion, and complexation with cyclodextrins have been utilized to resolve such problems. Indeed, in some selected cases, these approaches have been successful but they offer many other disadvantages. The main problem with micronization is chemical/thermal stability; many drugs may degrade and lose bioactivity when they are micronized by a conventional method. For solid dispersion, the amount of carriers used is often large, and thus if the dose of the active ingredient is high, the tablets or capsules formed will be large in volume and difficult to swallow. Moreover, the carriers used are usually expensive and the freeze-drying or spray-drying method requires particular facilities and processes, leading to a high production cost. Though a traditional solvent method can be adopted instead, it is difficult to deal with co-precipitates with a high viscosity. Complexation with cyclodextrins techniques is not applicable for drug substances which are not soluble in both aqueous and organic solvents. The realization that the oral bioavailability of poor water-soluble drugs may be enhanced when co-administered with a meal rich in fat has led to increasing recent interest in the formulation of poorly water soluble drugs in lipids. Lipid suspension, solutions, and emulsions have all been used to enhance the oral bioavailability, but more recently there have been much focus on the utility of a self-nanoemulsifying drug delivery system (SNEDDS). Being hydrophobic, i.e., more lipophilic, a lipid-based drug delivery system would ideally work for a poorly water soluble drug. Lipid-based drug delivery systems have gained considerable interest after the commercial success of Sandimmune Neoral (cyclosporine A), Fortovase (saquinavir) and Norvir (ritonavir).[ 2 – 5 ]
SNEDDS are defined as isotropic mixtures of natural or synthetic oils, solid or liquid surfactants, or alternatively, one or more hydrophilic solvents and cosolvents/surfactants that have the ability of forming fine oil-in-water (o/w) micro emulsions upon mild agitation followed by dilution in aqueous media, such as GI fluids. SNEDDS spread readily in the GI tract, and the digestive motility of the stomach and the intestine provides the agitation necessary for self-emulsification.
TEL displaces angiotensin II from the angiotensin I receptor and produces the blood pressure-lowering effects by antagonizing angiotensin II-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water intake, and hypertrophic response. TEL is practically insoluble in water (0.0035 mg/mL) and has high hydrophobicity (log P 6.66) with only 42% oral bioavailability. Hence, TEL was selected as a model drug for this study. TEL is available in various doses (20 mg, 40 mg, 80 mg and 120 mg); for our study a 20-mg dose was selected as a working dose to limit the total formulation volume. The aim of this study was to develop a SNEDDS containing a poor water soluble drug (telmisartan).
Telmisartan was obtained as a gift sample from Torrent Research Center, Bhat, Gandhinagar, Gujarat, India. The following materials were donated by Abitec Corp., USA, and were used as received: Acconon ® CC 400 (polyoxyethylene 6 capric esters), Acconon ® Sorb 20 (polyoxyethylene 20 sorbitol), Acconon ® E (polyoxypropylene 15 stearyl ether), Capmul ® MCM (glycerol mono-dicaprylate), Capmul ® GMO (glycerol mono/di-oleate), Capmul ® MCM C8, Captex ® 355 (caprylic/capric acid triglycerides) and Caprol ® ET (polyglycerol esters). Cremophor ® RH 40 (polyoxyl 40 hydrogenated castor oil) and Solutol ® HS 15 (macrogol 15 hydroxystearate) were also donated from BASF, Mumbai, Maharashtra, India. Miglylol ® 812 (caprylic/capric acid triglycerides) and Imwitor ® 742 (glycerol monocaprylocaprate) were generously gifted from Sasol, Germany. Sefsol ® 218 (propylene glycerol monocaprylate) was gifted from Nikko Chemicals, Tokyo, Japan. Labrafil ® M 2125 CS (linoleoyl macrogolglycerides), Plurol Oleique ® (polyglycerol oleate), and Capryol ® 90 (polypropylene glycol monocaprylate) were received as a gift sample from Gettefosse, Mumbai, Maharashtra, India. Acrysol ® K 140 (polyoxyl 40 hydrogenated castor oil) and Acrysol ® EL 135 (polyoxyl 35 castor oil) were also gifted from Corel Pharma, Gujarat, India. Cremophor ® EL (polyethoxylated castor oil) was purchased from Sigma Aldrich, India. Other chemicals like Span ® 20 (sorbitan monolaurate), Span ® 80 (sorbitan monooleate), Tween ® 20 (polyoxyethylene sorbitan monolaurate), Tween ® 80 (polyoxyethylene sorbitan monooleate), polyethylene glycol 400 (PEG 400), polyethylene glycol 200 (PEG 200), propylene glycol (PG), Carbitol ® (monoethyl ether of diethylene glycol), glycerol, castor oil, olive oil, cotton seed oil, poloxamer 188, and poloxamer 407 were bought from Merck India, Mumbai, and S. D. Fine Chem, Mumbai, Maharashtra, India. Double distilled water was used throughout the study. Acetonitrile and methanol used in the present study were of high-performance liquid chromatography (HPLC) grade. All other chemicals were reagent grade. Empty, hard gelatin capsule shells were generously donated by Torrent Research Center, Gujarat, India.
Male Wister rats (weighing approximately 250 ± 30 g) were used for the bioavailability studies. The animals were maintained at temperature (24–25°C), and humidity (60%), and were supplied with food and water ad libitum. The animal requirement was approved by the Institute Animal Ethics Committee (IAEC) and all experiments were conducted as per the norms of the Committee for the Purpose of Supervision of Experiments on Animals, India.
0The solubility of TEL in various buffers, oils, surfactants, and co-surfactants was measured using the shake flask method as suggested by Date and Nagarsenker. An excess amount of TEL was introduced into each excipient (2 mL) followed by sealing in vials. A vortex mixer (REMI, Mumbai, India) was used to facilitate the solubilization. Sealed vials were stirred in a water bath at 40°C for 24 h and allowed for reaching equilibrium at 30°C for 72 h. Each vial was centrifuged at 15,000 rpm for 10 min using a centrifuge (REMI, Mumbai, India) followed by the removal of undissolved TEL by filtering with a membrane filter (0.45 μ m). Samples were suitably diluted with methanol and a drug concentration was obtained via a validated UV method at 297 nm using methanol as a blank ( R 2 = 0.99057, %error = 1.5, CV = 2%, linearity = 1–20 μ g/mL) using a double-beam UV visible spectrophotometer (Shimadzu 1700, Shimadzu Corporation, Japan). The experiment was repeated in triplicates. Results were represented as mean values (mg/mL ± SD).
Different surfactants (Cremophor ® EL, Cremophor ® RH 40,
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