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Teaima, Mahmoud
- Formulation and In-vitro Characterization of Self Nano-emulsifying Drug Delivery System (SNEDDS) for enhanced Solubility of Candesartan Cilexetil
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Authors
Affiliations
1 Department of Pharmaceutics and Pharmaceutical Technology, Heliopolis University in Egypt, 3 Belbeis – Cairo Desert Road,Cairo, EG
1 Department of Pharmaceutics and Pharmaceutical Technology, Heliopolis University in Egypt, 3 Belbeis – Cairo Desert Road,Cairo, EG
Source
Research Journal of Pharmacy and Technology, Vol 12, No 6 (2019), Pagination: 2628-2636Abstract
Candesartan cilexetil is the prodrug of candesartan, a selective angiotensin II receptor antagonist, used in the management of hypertension and heart failure. It is characterized by poor aqueous solubility resulting in low bioavailability. Self-nanoemulsifying drug delivery systems (SNEDDS) loaded with candesartan cilexetil were successfully developed to overcome such obstacles. Preliminary screening was carried out to select proper oil, surfactant and co-surfactant combination for successful SNEDDS formulation. Ternary and pseudo ternary diagrams were constructed to optimize the system. Capryol 90® as an oil showed high emulsification ability. The nature of obtained dispersions was found to be nanoemulsions. Six formulations were visually inspected and evaluated for stability, robustness to dilution, effect of drug loading on the nano-emulsion boundary, viscosity, content uniformity, their mean droplet size, polydispersity index (PDI), zeta potential in addition to in vitro drug release study. Three formulations showed a very short emulsification time of less than 3minutes. The emulsification efficiency was significantly superior at pH6.8. All selected formulations showed mean droplet size (124.25 to 460.15nm), very low PDI values (0.311-0.562) and zeta potential (30.5-44.45 mV). Formulation F16 (10% w/w Capryol 90®, 30% w/w Tween80, 60% w/w Transcutol®) was selected for further characterization. Droplet size of F16 showed robustness to different dilution folds with different media. These results indicate that, SNEDDS could be promising delivery systems with a rapid onset of action and prolonged therapeutic effect of candesartan cilexetil.Keywords
Candesartan Cilexetil, SNEDDS, Capryol 90, Transcutol HP.
References
- Krumholz, H. M. et al. ACC/AHA Clinical Performance Measures for Adults With ST-Elevation and Non{textendash}ST-Elevation Myocardial Infarction. J. Am. Coll. Cardiol.47, 236–265 (2006).
- Patel, J. N., Rathod, D. M., Patel, N. A. and Modasiya, M. K. Techniques to improve the solubility of poorly soluble drugs. Int. J. Pharm. Life Sci.3, (2012).
- Rahman, A. et al. Oral lipidbased drug delivery system (LBDDS): formulation, characterization and application: a review. Curr. Drug Deliv.8, 330–345 (2011).
- Birajdar, G. O. et al. A Comprehensive Review on Nanotechnology. Res. J. Pharm. Technol.6, 3 (2013).
- Fathi, M., Mozafari, M.-R. and Mohebbi, M. Nanoencapsulation of food ingredients using lipid based delivery systems. Trends food Sci. Technol.23, 13–27 (2012).
- Sriram, K., Vishnupriya, V. and Gayathri, R. Review on the role of Nanotechnology in Dentistry and Medicine. Res. J. Pharm. Technol.9, 1249 (2016).
- Maravajhala, V., Papishetty, S. and Bandlapalli, S. Nanotechnology in development of drug delivery system. Int. J. Pharm. Sci. Res.3, 84 (2012).
- Vyas, A. and Gidwani, B. Technologies to Counter Poor Solubility Issues: A Review. Res. J. Pharm. Technol.6, 10 (2013).
- Muhamad12, I. I., Selvakumaran, S. and Lazim, N. A. M. Designing polymeric nanoparticles for targeted drug delivery system. Nanomed287, 287 (2014).
- Elgadira, M. A. and Adam, A. Selected drug delivery systems based on nanoemulsion. World J Pharm Res3, 1796–1809 (2014).
- Soni, G. C., Prajapati, S. K. and Chaudhri, N. Self nanoemulsion: advance form of drug delivery system. World J. Pharm. Pharm. Sci.3, 410–436 (2014).
- Varma, M. V, Ashokraj, Y., Dey, C. S. and Panchagnula, R. No Title. Pharmacol Res48, 347 (2003).
- Dey, S., Jha, S. K., Malakar, J. and Gangopadhyay, A. Improvement of bioavailability of poorly soluble drugs through self emulsifying drug delivery system. J. PharmaSciTech1, 6–11 (2012).
- Nekkanti, V., Karatgi, P., Prabhu, R. and Pillai, R. Solid selfmicroemulsifying formulation for candesartan cilexetil. AAPS PharmSciTech11, 9 (2010).
- Patel, M. J., Patel, S. S., Patel, N. M. and Patel, M. M. A selfmicroemulsifying drug delivery system (SMEDDS). Int J Pharm Sci Rev Res4, 29–35 (2010).
- Anagha, B., Shivanand, H., Manoj, A. and Poonam, P. Effect of lipids and surfactants on solid lipid nanoparticle engineering. Res. J. Pharm. Technol.4, 521–526 (2011).
- Wadhwa, J., Nair, A. and Kumria, R. Emulsion forming drug delivery system for lipophilic drugs. Acta Pol Pharm69, 179–191 (2012).
- Raghuveer, P., Vanithakamal, J., Madhuri, D. and Rani, A. P. Design development and evaluation of self nanoemulsifying drug delivery system of simvastatin. Res. J. Pharm. Technol.11, 1185–1192 (2018).
- Kalepu, S., Manthina, M. and Padavala, V. Oral lipid-based drug delivery systems--an overview. Acta Pharm. Sin. B3, 361–372 (2013).
- McClellan, K. J. and Goa, K. L. Candesartan cilexetil. A review of its use in essential hypertension. Drugs56, 847–869 (1998).
- Press, P. Martindale: the complete drug reference. Sweetman SC, London 29–31 (2009).
- Kolesar, J. M. and Vermeulen, L. C. Top 300 Pharmacy Drug Cards 2016-2017. (McGraw-Hill Education, 2016).
- Gao, F. et al. Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: Performance and mechanism. J. Control. Release149, 168–174 (2011).
- Gaurkhede, R. M. and Chandewar, A. V. Analytical Method Development and Validation for Simultaneous Estimation of Candesartan Cilexetil and Hydrochlorothiazide in Tablet Dosage form. Res. J. Pharm. Technol.11, 459–462 (2018).
- Kulsum, S., Sagar, G. V. and Padmalatha, M. Validated RP-HPLC Method for the Quantitation of Candesartan in Bulk and Pharmaceutical Dosage Forms. Res. J. Pharm. Technol.4, 997–998 (2011).
- Ratnaparkhi, M. P. Formulation and Evaluation of Sustained Release Floating Drug Delivery System of Candesartan Celexitil. Res. J. Pharm. Technol.7, 4 (2014).
- Agrawal, P. et al. Formulation and Evaluation of directly compressed Floating Tablets of Candesartan Cilexetil for Gastro Retentive Drug Delivery. Res. J. Pharm. Technol.11, 2804–2808 (2018).
- Dudhipala, N. and Veerabrahma, K. Candesartan cilexetil loaded solid lipid nanoparticles for oral delivery: characterization, pharmacokinetic and pharmacodynamic evaluation. Drug Deliv.23, 395–404 (2016).
- Zhou, L., Chen, X., Gu, Y. and Liang, J. No Title. Biopharm Drug Dispos30, 259 (2009).
- Gurunath, S., Nanjwade, B. K. and Patil, P. A. Oral bioavailability and intestinal absorption of candesartan cilexetil: Role of naringin as P-glycoprotein inhibitor. Drug Dev. Ind. Pharm.41, 170–176 (2015).
- Surampalli, G., Nanjwade, B. K. and Patil, P. A. Corroboration of naringin effects on the intestinal absorption and pharmacokinetic behavior of candesartan cilexetil solid dispersions using in-situ rat models. Drug Dev. Ind. Pharm.41, 1057–1065 (2015).
- Darwhekar, G. N., Jain, D. K. and Chouhan, J. Biopharmaceutical classification of candesartan and candesartan cilexetil. Asian J. Pharm. Life Sci. ISSN2231, 4423 (2012).
- Beale, J. M., Block, J. and Hill, R. Organic medicinal and pharmaceutical chemistry. (Lippincott Williams and Wilkins Philadelphia, 2010).
- Moffat, A. C., Osselton, M. D., Widdop, B. and Watts, J. Clarke’s analysis of drugs and poisons. 3, (Pharmaceutical press London, 2011).
- Rahman, M. A., Iqbal, Z. and Hussain, A. Formulation optimization and in vitro characterization of sertraline loaded self-nanoemulsifying drug delivery system (SNEDDS) for oral administration. J. Pharm. Investig.42, 191–202 (2012).
- Husain, A., Azim, M. S., Mitra, M. and Bhasin, P. S. A review on candesartan: pharmacological and pharmaceutical profile. J. Appl. Pharm. Sci.1, 12–17 (2011).
- Date, A. A. and Nagarsenker, M. S. Design and evaluation of selfnanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int. J. Pharm.329, 166–172 (2007).
- Chella, N., Shastri, N. and Tadikonda, R. R. Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan. Acta Pharm. Sin. B2, 502–508 (2012).
- Jaiswal, P., Aggarwal, G., Harikumar, S. L. and Singh, K. Development of self-microemulsifying drug delivery system and solid-self-microemulsifying drug delivery system of telmisartan. Int. J. Pharm. Investig.4, 195 (2014).
- Narkhede, R. S., Gujar, K. N. and Gambhire, V. M. Design and evaluation of self-nanoemulsifying drug delivery systems for nebivolol hydrochloride. Asian J. Pharm. Free full text Artic. from Asian J Pharm. 8, (2014).
- Badawi, A. A., Sakran, W. S., Ramadan, M. A. and El-Mancy, S. M. S. Improvement of the microbiological activity of topical ketoconazole using microemulsion systems. J. Drug Deliv. Sci. Technol. 22, 473–478 (2012).
- Bari, A., Chella, N., Sanka, K., Shastri, N. R. and Diwan, P. V. Improved anti-diabetic activity of glibenclamide using oral self nano emulsifying powder. J. Microencapsul.32, 54–60 (2015).
- Goyal, U., Gupta, A., Rana, A. C. and Aggarwal, G. Self microemulsifying drug delivery system: a method for enhancement of bioavailability. Int. J. Pharm. Sci. Res.3, 66 (2012).
- Mohd, A. B., Sanka, K., Bandi, S., Diwan, P. V and Shastri, N. Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits. Drug Deliv.22, 499–508 (2015).
- Basalious, E. B., Shawky, N. and Badr-Eldin, S. M. SNEDDS containing bioenhancers for improvement of dissolution and oral absorption of lacidipine. I: development and optimization. Int. J. Pharm.391, 203–211 (2010).
- Abdelbary, G., Amin, M. and Salah, S. Self nano-emulsifying simvastatin based tablets: design and in vitro/in vivo evaluation. Pharm. Dev. Technol.18, 1294–1304 (2013).
- Kale, A. A. and Patravale, V. B. Design and evaluation of selfemulsifying drug delivery systems (SEDDS) of nimodipine. AAPS PharmSciTech9, 191–196 (2008).
- Elmancy, S. M. S. Improvement of the performance of some hydrophobic drugs using lipid-based drug delivery systems. (2013).
- Shukla, J. B. and Patel, S. J. Formulation and evaluation of self micro emulsifying system of candesartan cilexetil. Int J Pharm Pharm Sci2, 143–146 (2010).
- Kaur, G., Chandel, P. and Harikumar, S. L. Formulation Development of Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Celecoxib for Improvement of Oral Bioavailability. Pharmacophore4, 120–133 (2013).
- Gupta, A. K., Mishra, D. K. and Mahajan, S. C. Preparation and invitro evaluation of self emulsifying drug delivery system of antihypertensive drug valsartan. Int. J. Pharm. Life Sci2, 633–639 (2011).
- Khamkar, G. S. Self micro-emulsifying drug delivery system (SMEDDS) o/w microemulsion for BCS Class II drugs: An approach to enhance an oral bioavailability. Int. J. Pharm. Pharm. Sci.3, 1–3 (2011).
- Wankhade, V., Pande, S., Tapar, K. and Bobade, N. Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDS) for Gliclazide. Der Pharm. Lett2, 132–143 (2010).
- Beg, S., Swain, S., Singh, H. P., Patra, C. N. and Rao, M. E. B. Development, optimization, and characterization of solid selfnanoemulsifying drug delivery systems of valsartan using porous carriers. AAPS pharmscitech13, 1416–1427 (2012).
- British Pharmacopoeia, B. P. and UK, H. M. The stationary office. (2008).
- Kumar, A. A., Sujathakumara, M., Surekha, K. and Prasad ChSS, S. S. Formulation and evaluation of sustained release Valsartan matrix tablets by using natural polymers. Int J Pharm Chem Biol Sci2, 146– 150 (2012).
- Kang, B. K. et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pharm.274, 65–73 (2004).
- Chengaiah, B., Alagusundaram, M., Ramkanth, S. and Madhusudhana, C. C. Self-emulsifying drug delivery system: a novel approach for drug delivery. Res. J. Pharm. Technol.4, 175–181 (2011).
- Tang, S. Y., Manickam, S., Wei, T. K. and Nashiru, B. Formulation development and optimization of a novel Cremophore EL-based nanoemulsion using ultrasound cavitation. Ultrason. Sonochem.19, 330–345 (2012).
- Maged, A., Mahmoud, A. A. and Ghorab, M. M. Nano spray drying technique as a novel approach to formulate stable econazole nitrate nanosuspension formulations for ocular use. Mol. Pharm.13, 2951– 2965 (2016).
- Maged, A., Mahmoud, A. A. and Ghorab, M. M. Hydroxypropylbetacyclodextrin as cryoprotectant in nanoparticles prepared by nano-spray drying technique. J. Pharm. Sci. Emerg. Drugs2017, (2017).
- Muñoz-Cernada, A. et al. Effect of nonionic surfactants and HPMC F4M on the development of formulations of Neuro-EPO as a neuroprotective agent. J. Adv. Pharm. Sci. Technol.1, 22 (2014).
- Mohsin, K., Rayan Alamri, A. A., Raish, M., Alanazi, F. K. and Hussain, M. D. Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug. Int. J. Nanomedicine11, 2829 (2016).
- Shafiq-un-Nabi, S. et al. Formulation development and optimization using nanoemulsion technique: a technical note. AAPS pharmscitech8, E12--E17 (2007).
- Hyma, P., Reddy, L. and Neelima, D. Formulation and Evaluation of a Self Microemulsifying Drug Delivery System of Atorvastatin Calcium Trihydrate. Res. J. Pharm. Technol.9, 789 (2016).
- Mahmoud, E. A., Bendas, E. R. and Mohamed, M. I. Preparation and evaluation of self-nanoemulsifying tablets of carvedilol. AAPS pharmscitech10, 183–192 (2009).
- Salimi, A., Zadeh, B. S. M., asghar Hemati, A. and Birgani, S. A. Design and evaluation of self-emulsifying drug delivery system (SEDDS) of carvedilol to improve the oral absorption. Jundishapur J. Nat. Pharm. Prod.9, (2014).
- Oh, D. H. et al. Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier. Int. J. Pharm.420, 412–418 (2011).
- Wu, X., Xu, J., Huang, X. and Wen, C. Self-microemulsifying drug delivery system improves curcumin dissolution and bioavailability. Drug Dev. Ind. Pharm.37, 15–23 (2011).
- Dixit, A. R., Rajput, S. J. and Patel, S. G. Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS pharmscitech11, 314–321 (2010).
- Gumaste, S. G., Dalrymple, D. M. and Serajuddin, A. T. M. Development of solid SEDDS, V: compaction and drug release properties of tablets prepared by adsorbing lipid-based formulations onto Neusilin®US2. Pharm. Res.30, 3186–3199 (2013).
- Eid, A. M. M., Baie, S. H. and Arafat, O. M. The effect of surfactant blends on the production of self-emulsifying system. Int. J. Pharm. Front. Res2, 21–31 (2012).
- Nawale, R. B. and Mehta, B. N. Glibenclamide loaded selfmicroemulsifying drug delivery system (SMEDDS): development and optimization. Int J Pharm Pharm Sci5, 325–330 (2013).
- Marasini, N. et al. Development and optimization of selfnanoemulsifying drug delivery system with enhanced bioavailability by Box--Behnken design and desirability function. J. Pharm. Sci.101, 4584–4596 (2012).
- Buyukozturk, F., Benneyan, J. C. and Carrier, R. L. Impact of emulsion-based drug delivery systems on intestinal permeability and drug release kinetics. J. Control. release142, 22–30 (2010).
- Shanmugam, S. et al. Solid self-nanoemulsifying drug delivery system (S-SNEDDS) containing phosphatidylcholine for enhanced bioavailability of highly lipophilic bioactive carotenoid lutein. Eur. J. Pharm. Biopharm.79, 250–257 (2011).
- Manohari, P. J., Kunchitapatham, J., Seshadri, V. C. and Muthusamy, C. Development of self micro emulsifying drug delivery system: application to pimozide delivery. Der Pharm Sin4, 48–58 (2013).
- Ranade, S., Londhe, V. and Bajaj, A. Microemulsion based gels for targeting neuropathic pain. Int J Pharm Sci Res5, 2525–2534 (2014).