ENHANCING OF ORAL BIOAVAILABILITY OF POORLY WATER-SOLUBLE ANTIHYPERTENSIVE DRUGS
DOI:
https://doi.org/10.22159/ijcpr.2021v13i4.42741Keywords:
Nanoparticles, Anti-hypertension, Hydrophobic drugs, Oral bioavailability, NanocarriersAbstract
Among various routes of drug delivery, Oral administration is the most convenient route because of its high patient compliance. Although oral drug delivery is effective for drugs with high aqueous solubility and epithelial permeability; however for poorly aqueous soluble drug the membrane permeability, chemical, and enzymatic stability of drugs are the major limitations in successful oral drug delivery. Almost 70% of the new drug candidates which shows poor bioavailability, the antihypertensive drugs are among those. Novel drug delivery systems are available in many areas to overcome the problems associated with hydrophobic drugs and the nanotechnology-based drug delivery system is the most potential to beat the challenges related to the oral route of administration with some important advantages such as the colloidal size, biocompatibility, lowered dose size, reduced toxicity, patient compliance and drug targeting. The foremost common nanotechnology-based strategies utilized in the development of delivery systems are nano-emulsions, nano-suspensions, dendrimers, micelles, liposomes, solid lipid nanoparticles, polymeric nanoparticles, carbon nanotubes, Self-Nano-emulsifying Drug Delivery System, proliposomes, nano-crystals, and so forth, which give controlled, sustained, and targeted drug delivery. The appliance of those systems within the treatment of hypertension continues to broaden. This review focuses on various nano-carriers available in oral drug administration for improving solubility profile, dissolution, and consequently bioavailability of hydrophobic antihypertensive drugs.
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References
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33. Parveen S, Misra R, Sahoo SK. Nanoparticles: a boon to drug delivery, therapeutics, diagnostics and imaging. Nanomed Nanotechnol Biol Med 2012;8:147–66.
34. Patel J, Dhingani A, Garala K, Raval M, Sheth N. Design and development of solid nanoparticulate dosage forms of telmisartan for bioavailability enhancement by integration of experimental design and principal component analysis. Powder Technol 2014;258:331–43.
35. Liu D, Yu S, Zhu Z, Lyu C, Bai C, Ge H, et al. Controlled delivery of carvedilol nanosuspension from osmotic pump capsule: in vitro and in vivo evaluation. Int J Pharm 2014;475:496–503.
36. Thakar D, Bharadia P, Pandya V. Enhancement of solubility of poorly water-soluble antihypertensive drug by nanosizing approach. J Pharm Bioallied Sci 2012;4(Suppl):40–1.
37. Thadkala K, Sailu C, Aukunuru J. Formulation, optimization and evaluation of oral nanosuspension tablets of nebivolol hydrochloride for enhancement of dissolution rate. Der Pharm Lett 2015;7:71–84.
38. Vidyanikethan S. Design and characterization of valsartan nano suspension. Int J Pharmacother 2012;2:70-81.
39. Sahu BP, Das MK. Nanosuspension for enhancement of oral bioavailability of felodipine. Appl Nanosci 2014;4:189–97.
40. Detroja C, Chavhan S, Sawant K. Enhanced antihypertensive activity of candesartan cilexetil nanosuspension: formulation, characterization and pharmacodynamic study. Sci Pharm 2011;79:635–51.
41. Solans C, Sole I. Nano-emulsions: formation by low-energy methods. Curr Opin Colloid Interface Sci 2012;17:246–54.
42. Ghai D, Sinha VR. Nanoemulsions as self-emulsified drug delivery carriers for enhanced permeability of the poorly water-soluble selective ?1-adrenoreceptor blocker talinolol. Nanomed Nanotechnol Biol Med 2012;8:618–26.
43. Gorain B, Choudhury H, Kundu A, Sarkar L, Karmakar S, Jaisankar P, et al. Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats. Colloids Surf B 2014;115:286–94.
44. Guan J, Zhao N, Zhai Y, Chu C, Chen H, Zhang T. Pharmacokinetic performance of the nitrendipine intravenous submicron emulsion in rats. Asian J Pharm Sci 2014;9:330–5.
45. Rajinikanth PS, Keat NW, Garg S. Self-nanoemulsifying drug delivery systems of valsartan: preparation and in vitro characterization. Int J Drug Delivery 2012;4:153–63.
46. Gupta AK. MDK and MSC. Delivery system of antihypertensive drug valsartan. Int J Pharm Life Sci 2011;2:633–9.
47. Mohanraj VJ, Chen Y. Nanoparticles-a review. Trop J Pharm Res 2007;5:561–73.
48. Mudshinge SR, Deore AB, Patil S, Bhalgat CM. Nanoparticles: emerging carriers for drug delivery. Saudi Pharm J 2011;19:129–41.
49. Ochekpe NA, Olorunfemi PO, Ngwuluka NC. Nanotechnology and drug delivery part 2: nanostructures for drug delivery. Trop J Pharm Res 2009;8:275–87.
50. Zhang L, Webster TJ, Zdrojewicz Z, Waracki M, Bugaj B, Pypno D, et al. Nanotechnology in therapeutics: a focus on nanoparticles as a drug delivery system R eview. Carbohydr Polym 2016;1:71–88.
51. Rao JP, Geckeler KE. Polymer nanoparticles: preparation techniques and size-control parameters. Prog Polym Sci 2011;36:887–913.
52. Jong WH De, Paul JB. Drug delivery and nanoparticles: applications and hazards. Int J Nanomed 2008;3:133–49.
53. Sinica DP, Bharathi M, Chandra S, Prasad M, Eswari RL, Raja SW, et al. Preparation and in vitro and in vivo characterization of valsartan loaded eudragit nanoparticles. Der Pharm Sin 2012;3:516–25.
54. Verger ML Le, Fluckiger L, Kim Y Il, Hoffman M, Maincent P. Preparation and characterization of nanoparticles containing an antihypertensive agent. Eur J Pharm Biopharm 1998;46:137–43.
55. Zhang Y, Jiang T, Zhang Q, Wang S. Inclusion of telmisartan in mesocellular foam nanoparticles: drug loading and release property. Eur J Pharm Biopharm 2010;76:17–23.
56. Jana U, Mohanty AK, Manna PK, Mohanta GP. Preparation and characterization of nebivolol nanoparticles using Eudragit® RS100. Colloids Surf B 2014;113:269–75.
57. Li F, Zhu A, Song X, Ji L. Novel surfactant for preparation of poly(l-lactic acid) nanoparticles with controllable release profile and cytocompatibility for drug delivery. Colloids Surf B 2014;115:377–83.
58. Kumar L, Sreenivasa Reddy M, Managuli RS, Pai KG. Full factorial design for optimization, development and validation of HPLC method to determine valsartan in nanoparticles. Saudi Pharm J 2015;23:549–55.
59. Kim Y Il, Fluckiger L, Hoffman M, Lartaud Idjouadiene I, Atkinson J, Maincent P. The antihypertensive effect of orally administered nifedipine-loaded nanoparticles in spontaneously hypertensive rats. Br J Pharmacol 1997;120:399–404.
60. Zheng X, Wang T, Jiang H, Li Y, Jiang T, Zhang J, et al. Incorporation of carvedilol into PAMAM-functionalized MWNTs as a sustained drug delivery system for enhanced dissolution and drug-loading capacity. Asian J Pharm Sci 2013;8:278–86.
61. Wong BS, Yoong SL, Jagusiak A, Panczyk T, Ho HK, Ang WH, et al. Carbon nanotubes for delivery of small molecule drugs. Adv Drug Delivery Rev 2013;65:1964–2015.
62. Arzani G, Haeri A, Daeihamed M, Bakhtiari Kaboutaraki H, Dadashzadeh S. Niosomal carriers enhance oral bioavailability of carvedilol: Effects of bile salt-enriched vesicles and carrier surface charge. Int J Nanomed 2015;10:4797–813.
63. Junyaprasert VB, Morakul B. Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs. Asian J Pharm Sci 2015;10:13–23.
64. Hecq J, Deleers M, Fanara D, Vranckx H, Amighi K. Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine. Int J Pharm 2005;299:167–77.
65. Quan P, Shi K, Piao H, Piao H, Liang N, Xia D, et al. A novel surface modified nitrendipine nanocrystals with an enhancement of bioavailability and stability. Int J Pharm 2012;430:366–71.
66. Quan P, Xia D, Piao H, Piao H, Shi K, Jia Y, et al. Nitrendipine nanocrystals: its preparation, characterization, and in vitro-in vivo evaluation. AAPS PharmSciTech 2011;12:1136–43.
67. Fu Q, Sun J, Ai X, Zhang P, Li M, Wang Y, et al. Nimodipine nanocrystals for oral bioavailability improvement: role of mesenteric lymph transport in the oral absorption. Int J Pharm 2013;448:290–7.
68. Hildebrand A, Beyer K, Neubert R, Garidel P, Blume A. Temperature dependence of the interaction of cholate and deoxycholate with fluid model membranes and their solubilization into mixed micelles. Colloids Surf B 2003;32:335–51.
69. Bobbala SKR, Veerareddy PR. Formulation, evaluation, and pharmacokinetics of isradipine proliposomes for oral delivery. J Liposome Res 2012;22:285–94.
70. Song KH, Chung SJ, Shim CK. Preparation and evaluation of proliposomes containing salmon calcitonin. J Controlled Release 2002;84:27–37.
71. Taylor P, Nekkanti V, Venkatesan N, Wang Z, Betageri GV, Nekkanti V, et al. Improved oral bioavailability of valsartan using proliposomes: design, characterization and in vivo pharmacokinetics improved oral bioavailability of valsartan using proliposomes: design, characterization and in vivo pharmacokinetics. Drug Dev Ind Pharm 2015;41:2077-88.
2. Sharma M, Sharma R, Jain DK. Nanotechnology-based approaches for enhancing oral bioavailability of poorly water-soluble antihypertensive drugs. Scientifica 2016. DOI:10.1155/2016/8525679
3. Khadka P, Ro J, Kim H, Kim I, Kim JT, Kim H, et al. Pharmaceutical particle technologies: an approach to improve drug solubility, dissolution and bioavailability. Asian J Pharm Sci 2014;9:304–16.
4. Vikas K, Arvind S, Ashish S, Gourav J, Vipasha D. Recent advances in Ndds (novel drug delivery system) for delivery of anti-hypertensive drugs. Int J Drug Dev Res 2011;3:252–9.
5. Prisant LM, Elliott WJ. Drug delivery systems for treatment of systemic hypertension. Clin Pharmacokinet 2003;42:931-40.
6. Delmar K, Bianco Peled H. Composite chitosan hydrogels for extended-release of hydrophobic drugs. Carbohydr Polym 2016;136:570–80.
7. Gupta H, Bhandari D, Sharma A. Recent trends in oral drug delivery: a review. Recent Pat Drug Delivery Formul 2009;3:162–73.
8. Patwekar SL, Baramade MK. Controlled release approach to novel multiparticulate drug delivery system. Int J Pharm Pharm Sci 2012;4(Suppl 3):757–63.
9. Safari J, Zarnegar Z. Advanced drug delivery systems: nanotechnology of health design a review. J Saudi Chem Soc 2014;18:85–99.
10. Kalepu S, Nekkanti V. Insoluble drug delivery strategies: a review of recent advances and business prospects. Acta Pharm Sin B 2015;5:442–53.
11. G SR, Lakshmi P, Manjula E. Available online through phytopathogens. Plant Pathog 2010;1:114–7.
12. Gupta AK, Sehrawat SK. Bioavailability enhancement of poorly water-soluble drugs: a review. Int J Pharm Life Sci 2011;2:640–50.
13. Suri SS, Fenniri H, Singh B. Nanotechnology-based drug delivery systems. J Occup Med Toxicol 2007;2:1–6.
14. Shaji J, Bhatia V. Novel lipid carriers for oral delivery of lipophilic drugs. Int J Pharm Sci Rev Res 2012;15:47–53.
15. Mei L, Zhang Z, Zhao L, Huang L, Yang XL, Tang J, et al. Pharmaceutical nanotechnology for oral delivery of anticancer drugs. Adv Drug Delivery Rev 2013;65:880–90.
16. Mukherjee S, Ray S, Thakur RS. Solid lipid nanoparticles: A modern formulation approach in drug delivery system. Indian J Pharm Sci 2009;71:349–58.
17. Yadav N, Khatak S, Singh Sara UV. Solid lipid nanoparticles-a review. Int J Appl Pharm 2013;5:8–18.
18. Venishetty VK, Chede R, Komuravelli R, Adepu L, Sistla R, Diwan PV. Design and evaluation of polymer-coated carvedilol loaded solid lipid nanoparticles to improve the oral bioavailability: a novel strategy to avoid intraduodenal administration. Colloids Surf B 2012;95:1–9.
19. Kumar VV, Chandrasekar D, Ramakrishna S, Kishan V, Rao YM, Diwan PV. Development and evaluation of nitrendipine loaded solid lipid nanoparticles: influence of wax and glyceride lipids on plasma pharmacokinetics. Int J Pharm 2007;335:167–75.
20. Ekambaram P, Abdul Hasan Sathali A. Formulation and evaluation of solid lipid nanoparticles of ramipril. J Young Pharm 2011;3:216–20.
21. Sawant KK, Parmar B, Mandal SA, Petkar KC, Patel LD. Valsartan loaded solid lipid nanoparticles: development, characterization, and in vitro and ex vivo evaluation. Int J Pharm Sci Nanotechnol 2011;4:1483–90.
22. Kaur M. Dendrimers: synthesis, its dosage forms and advantage over linear polymers. Mintage J Pharm Med Sci 2014;3:15–9.
23. Dwivedi DK, Singh AK. Dendrimers: a novel carrier system for drug delivery. J Drug Delivery Ther 2014;4:1–6.
24. Kesharwani P, Jain K, Jain NK. Dendrimer as a nanocarrier for drug delivery. Prog Polym Sci 2014;39:268–307.
25. Nanjwade BK, Bechra HM, Derkar GK, Manvi FV, Nanjwade VK. Dendrimers: emerging polymers for drug-delivery systems. Eur J Pharm Sci 2009;38:185–96.
26. Tripathy S, Das MK. Dendrimers and their applications as novel drug delivery carriers. J Appl Pharm Sci 2013;3:142–9.
27. Yu M, Jie X, Xu L, Chen C, Shen W, Cao Y, et al. Recent advances in dendrimer research for cardiovascular diseases. Biomacromolecules 2015;16:2588–98.
28. Jain NK, Tekade RK. Dendrimers for enhanced drug solubilization. Drug Delivery Strateg Poorly Water-Soluble Drugs 2013;3:373–409.
29. Info A. Pamam dendrimers: novel polymeric nanoarchitectures for solubility enhancement of candesartan cilexetil. Res Gate: Pharm Sci 2012;1:1–4.
30. Sica DA. Pharmacotherapy review: calcium channel blockers. J Clin Hypertens (Greenwich) 2006;8:53–6.
31. D’Emanuele A, Jevprasesphant R, Penny J, Attwood D. The use of a dendrimer-propranolol prodrug to bypass efflux transporters and enhance oral bioavailability. J Controlled Release 2004;95:447–53.
32. Devarakonda B, Li N, de Villiers MM. Effect of polyamidoamine (PAMAM) dendrimers on the in vitro release of water-insoluble nifedipine from aqueous gels. AAPS PharmSciTech 2005;6:504–12.
33. Parveen S, Misra R, Sahoo SK. Nanoparticles: a boon to drug delivery, therapeutics, diagnostics and imaging. Nanomed Nanotechnol Biol Med 2012;8:147–66.
34. Patel J, Dhingani A, Garala K, Raval M, Sheth N. Design and development of solid nanoparticulate dosage forms of telmisartan for bioavailability enhancement by integration of experimental design and principal component analysis. Powder Technol 2014;258:331–43.
35. Liu D, Yu S, Zhu Z, Lyu C, Bai C, Ge H, et al. Controlled delivery of carvedilol nanosuspension from osmotic pump capsule: in vitro and in vivo evaluation. Int J Pharm 2014;475:496–503.
36. Thakar D, Bharadia P, Pandya V. Enhancement of solubility of poorly water-soluble antihypertensive drug by nanosizing approach. J Pharm Bioallied Sci 2012;4(Suppl):40–1.
37. Thadkala K, Sailu C, Aukunuru J. Formulation, optimization and evaluation of oral nanosuspension tablets of nebivolol hydrochloride for enhancement of dissolution rate. Der Pharm Lett 2015;7:71–84.
38. Vidyanikethan S. Design and characterization of valsartan nano suspension. Int J Pharmacother 2012;2:70-81.
39. Sahu BP, Das MK. Nanosuspension for enhancement of oral bioavailability of felodipine. Appl Nanosci 2014;4:189–97.
40. Detroja C, Chavhan S, Sawant K. Enhanced antihypertensive activity of candesartan cilexetil nanosuspension: formulation, characterization and pharmacodynamic study. Sci Pharm 2011;79:635–51.
41. Solans C, Sole I. Nano-emulsions: formation by low-energy methods. Curr Opin Colloid Interface Sci 2012;17:246–54.
42. Ghai D, Sinha VR. Nanoemulsions as self-emulsified drug delivery carriers for enhanced permeability of the poorly water-soluble selective ?1-adrenoreceptor blocker talinolol. Nanomed Nanotechnol Biol Med 2012;8:618–26.
43. Gorain B, Choudhury H, Kundu A, Sarkar L, Karmakar S, Jaisankar P, et al. Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats. Colloids Surf B 2014;115:286–94.
44. Guan J, Zhao N, Zhai Y, Chu C, Chen H, Zhang T. Pharmacokinetic performance of the nitrendipine intravenous submicron emulsion in rats. Asian J Pharm Sci 2014;9:330–5.
45. Rajinikanth PS, Keat NW, Garg S. Self-nanoemulsifying drug delivery systems of valsartan: preparation and in vitro characterization. Int J Drug Delivery 2012;4:153–63.
46. Gupta AK. MDK and MSC. Delivery system of antihypertensive drug valsartan. Int J Pharm Life Sci 2011;2:633–9.
47. Mohanraj VJ, Chen Y. Nanoparticles-a review. Trop J Pharm Res 2007;5:561–73.
48. Mudshinge SR, Deore AB, Patil S, Bhalgat CM. Nanoparticles: emerging carriers for drug delivery. Saudi Pharm J 2011;19:129–41.
49. Ochekpe NA, Olorunfemi PO, Ngwuluka NC. Nanotechnology and drug delivery part 2: nanostructures for drug delivery. Trop J Pharm Res 2009;8:275–87.
50. Zhang L, Webster TJ, Zdrojewicz Z, Waracki M, Bugaj B, Pypno D, et al. Nanotechnology in therapeutics: a focus on nanoparticles as a drug delivery system R eview. Carbohydr Polym 2016;1:71–88.
51. Rao JP, Geckeler KE. Polymer nanoparticles: preparation techniques and size-control parameters. Prog Polym Sci 2011;36:887–913.
52. Jong WH De, Paul JB. Drug delivery and nanoparticles: applications and hazards. Int J Nanomed 2008;3:133–49.
53. Sinica DP, Bharathi M, Chandra S, Prasad M, Eswari RL, Raja SW, et al. Preparation and in vitro and in vivo characterization of valsartan loaded eudragit nanoparticles. Der Pharm Sin 2012;3:516–25.
54. Verger ML Le, Fluckiger L, Kim Y Il, Hoffman M, Maincent P. Preparation and characterization of nanoparticles containing an antihypertensive agent. Eur J Pharm Biopharm 1998;46:137–43.
55. Zhang Y, Jiang T, Zhang Q, Wang S. Inclusion of telmisartan in mesocellular foam nanoparticles: drug loading and release property. Eur J Pharm Biopharm 2010;76:17–23.
56. Jana U, Mohanty AK, Manna PK, Mohanta GP. Preparation and characterization of nebivolol nanoparticles using Eudragit® RS100. Colloids Surf B 2014;113:269–75.
57. Li F, Zhu A, Song X, Ji L. Novel surfactant for preparation of poly(l-lactic acid) nanoparticles with controllable release profile and cytocompatibility for drug delivery. Colloids Surf B 2014;115:377–83.
58. Kumar L, Sreenivasa Reddy M, Managuli RS, Pai KG. Full factorial design for optimization, development and validation of HPLC method to determine valsartan in nanoparticles. Saudi Pharm J 2015;23:549–55.
59. Kim Y Il, Fluckiger L, Hoffman M, Lartaud Idjouadiene I, Atkinson J, Maincent P. The antihypertensive effect of orally administered nifedipine-loaded nanoparticles in spontaneously hypertensive rats. Br J Pharmacol 1997;120:399–404.
60. Zheng X, Wang T, Jiang H, Li Y, Jiang T, Zhang J, et al. Incorporation of carvedilol into PAMAM-functionalized MWNTs as a sustained drug delivery system for enhanced dissolution and drug-loading capacity. Asian J Pharm Sci 2013;8:278–86.
61. Wong BS, Yoong SL, Jagusiak A, Panczyk T, Ho HK, Ang WH, et al. Carbon nanotubes for delivery of small molecule drugs. Adv Drug Delivery Rev 2013;65:1964–2015.
62. Arzani G, Haeri A, Daeihamed M, Bakhtiari Kaboutaraki H, Dadashzadeh S. Niosomal carriers enhance oral bioavailability of carvedilol: Effects of bile salt-enriched vesicles and carrier surface charge. Int J Nanomed 2015;10:4797–813.
63. Junyaprasert VB, Morakul B. Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs. Asian J Pharm Sci 2015;10:13–23.
64. Hecq J, Deleers M, Fanara D, Vranckx H, Amighi K. Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine. Int J Pharm 2005;299:167–77.
65. Quan P, Shi K, Piao H, Piao H, Liang N, Xia D, et al. A novel surface modified nitrendipine nanocrystals with an enhancement of bioavailability and stability. Int J Pharm 2012;430:366–71.
66. Quan P, Xia D, Piao H, Piao H, Shi K, Jia Y, et al. Nitrendipine nanocrystals: its preparation, characterization, and in vitro-in vivo evaluation. AAPS PharmSciTech 2011;12:1136–43.
67. Fu Q, Sun J, Ai X, Zhang P, Li M, Wang Y, et al. Nimodipine nanocrystals for oral bioavailability improvement: role of mesenteric lymph transport in the oral absorption. Int J Pharm 2013;448:290–7.
68. Hildebrand A, Beyer K, Neubert R, Garidel P, Blume A. Temperature dependence of the interaction of cholate and deoxycholate with fluid model membranes and their solubilization into mixed micelles. Colloids Surf B 2003;32:335–51.
69. Bobbala SKR, Veerareddy PR. Formulation, evaluation, and pharmacokinetics of isradipine proliposomes for oral delivery. J Liposome Res 2012;22:285–94.
70. Song KH, Chung SJ, Shim CK. Preparation and evaluation of proliposomes containing salmon calcitonin. J Controlled Release 2002;84:27–37.
71. Taylor P, Nekkanti V, Venkatesan N, Wang Z, Betageri GV, Nekkanti V, et al. Improved oral bioavailability of valsartan using proliposomes: design, characterization and in vivo pharmacokinetics improved oral bioavailability of valsartan using proliposomes: design, characterization and in vivo pharmacokinetics. Drug Dev Ind Pharm 2015;41:2077-88.
Published
15-07-2021
How to Cite
BAISHYA, B., S. S. RAHMAN, D. RYNJAH, K. BARMAN, S. S. BORDOLOI, J. ISLAM, and N. HASAN. “ENHANCING OF ORAL BIOAVAILABILITY OF POORLY WATER-SOLUBLE ANTIHYPERTENSIVE DRUGS”. International Journal of Current Pharmaceutical Research, vol. 13, no. 4, July 2021, pp. 42-47, doi:10.22159/ijcpr.2021v13i4.42741.
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Review Article(s)
