Nanosuspension formulation & evaluation of ritonavir & valsartan by using poloxamer as a stabilizing agent to enhance the oral bio availability
Abstract
The Nano ionization technology is particularly promising for improving the oral absorption and bioavailability of BCS class II drugs. One such approach is Nano ionization thereby increasing surface area and hence dissolution and ultimately the bioavailability. Ritonavir is a BCS class II and IV drug. Valsartan is a commonly used antihypertensive agent belonging to the family of angiotensin II receptor antagonists. Valsartan is a BCS class II drug being slightly soluble in water. It has a very low oral bioavailability of 25-35% due to its limited solubility in biological fluids. Poor water solubility of drugs shows insufficient bioavailability and fluctuating plasmalevels. Based on their physicochemical and biopharmaceutical properties, Ritonavir and Valsartan were selected as a drug candidates for developing Nanosuspension based formulations for improving the solubility and bioavailability by enhancing the rate and extent ofdissolution.The scope of the present work is to enhance the solubility, dissolution rate and oral bio availability of poorly soluble drugs Ritonavir and Valsartan by formulating them into Nanosuspension with Poloxamer as a stabilizing agent and subsequently converting the optimized Nanosuspension of Ritonavir/Valsartan drug molecule into tablets and capsuleswith the help of various extragranular agents.
Keywords:
Valsartan, Ritonavir, BCS
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References
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Akhter S, Hossain I (2012). Dissolution enhancement of Capmul PG8 and Cremophor EL based Ibuprofen self emulsifying drug delivery system (SEDDS) using Response surface methodology, Int. Cur Pharm Journal, 1(6):138-150.
Amal S.M, Abu E.E, Gina S.E (2013). Formulation and evaluation in-situ gelling Tenoxicam liquid suppositories, Journal of life Medicine, 1(2):23-32.
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Amir H.F, Peter W (2009). Nanoparticles in cellular drug delivery, Bioorganic and med. Chemistry, 17:2950-2962.
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Bleich J, Muller B.W, Wabmus W (1993). Aerosol solvent extraction system-a new microparticle production technique, Int.. Journal of Pharmaceutics, 97(1):111-117.
Bo H, Thomas J.M, Christine D.K (2008). Nanowire sensors for multiplexed detection of biomolecules, Curr. Opin. Chem. Biology, 12(5):522-528.
Bohm B.H, Muller R.H (1999). Lab scale production unit design for Nanosuspensions of sparingly soluble cytotoxic drugs, Pharm. Sci. Techno. Today, 2:336-339.
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Brian W.G, Gina M.G, Lisa L. V.M, David J.G (1998). Analysis of Ritonavir in Plasma/Serum and Tissues by High- performance liquid chromatography, Journal of Pharm. and Toxi. methods, 40:235-239.
Briggs T. L, Maxwell T.J (1973). Process for preparing powder blends, US patent no 3721725.
Brunner E (1904). Reaktionsgeschwindigkeit in heterogenenSystemen, Journal of Phys. Chemistry, 47:56–102.
Buchi N.N, Ramya K.M, Peter A.C (2012). Effect of recrystallization on the pharmaceutical properties of Valsartan for improved therapeutic efficiency, Journal of Applied Pharm. Science, 2(10):126-132.
Ajay J.Y, Pradeep K.G, Vadahari B.N (2012). Sustain release Nanosuspension of Acetominophen- Formulation and invitro evaluation, Int. Journal of Research in Pharm Sciences, 3(1):67-71.
Akhter S, Hossain I (2012). Dissolution enhancement of Capmul PG8 and Cremophor EL based Ibuprofen self emulsifying drug delivery system (SEDDS) using Response surface methodology, Int. Cur Pharm Journal, 1(6):138-150.
Amal S.M, Abu E.E, Gina S.E (2013). Formulation and evaluation in-situ gelling Tenoxicam liquid suppositories, Journal of life Medicine, 1(2):23-32.
Amidon G.L, Lennernas H, Shah V.P, Crison J.R (1995). Theoritical basis for a biopharmaceutical drug classification: the correlation of invivobioavailability, Pharm. Research,413-420.
Amir H.F, Peter W (2009). Nanoparticles in cellular drug delivery, Bioorganic and med. Chemistry, 17:2950-2962.
Amit C, Upendra N, Neha G, Sharma V.K, Khosa R.L (2012). Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: A recent review, Journal of Adv. Pharm Edu. and Research, 2(1):32-67.
Andrej D, Julijana K, Sasa B, Odon P (2009). Advantages of Celecoxib Nanosuspension formulation and transformation into tablets, Int. Journal of pharmaceutics,376:204-212.
Anil kumar A, Sujatha kumari M, Surekha K, Prasad CHSS, Suresh S (2012). Formulation and evaluation of sustained release Valsartan matrix tablets by using natural polymers, Int. Journal of Pharm Chemical and Biological Sciences, 2(2):146-150.
Anilkumar J. S, Harinath N.M (2011). Design and evaluation of polylactic co-glycolic acid Nanoparticles containing Simvastatin, Int. Journal of Drug Devt. and Research, 3(2): 280-289.
Anwar K, Rishabha M, Pramod K.S (2014). A review on bioavailability enhancement techniques of poorly soluble drugs, Int. Journal of Pharmacy, 4(3):260-266.
Arne W.H, John S (1979). Evaluation of sodium sterarylfumerate as tablet lubricant, Int. Journal of Pharmaceutics, 2(3):145-153.
Arunkumar N, Deecaraman M, Rani C, Mohanraj K.P, Venkateshkumar K (2010). Formulation development and invitro evaluation of Nanosuspensions loaded with Atrovastatin Calcium, Asian Journal of Pharmaceutics, and 4(1):28-33.
Ashwini P.G, Nilesh V.K, Saptrishi D (2014). Review on enhancement of solubilization process, Am. Journal of Drug Discovery and Development, 4:134-152.
Banavath H (2010). Nanosuspension: an attempt to enhance bioavailability of poorly soluble drugs, Int. Journal of Pharm Sciences and Research, 1(9):1-11.
Bankar S.G, Rhodes C.T (1998). Disperse Systems: Modern pharmaceutics. 3rdaddition
Battu S.K, Repca M.A, Majumdar S, Madhusudan R.Y (2007). Formulation and evaluation of rapidly disintegrating Fenoverine tablets: effects of superdisintegrants, Drug Dev. Ind. Pharmacy, 33(11):1225-1232.
Becon N (2000) Nanoscience and Nanotechnology shaping biomedical research, symposium report, national institues of health bioengineering consortium,http://www.becon.nih.gov/nanotechsympreport.pdf.
Behera A.L, Patil S.V, Sahoo S. K (2010). Nanosizing of drugs: A promising approach for drug delivery, Der Pharmacia Sinica, 1(1):20-28.
Bentley M.V, Marchetti J.M, Ricardo N, Ali A. Z, Collett J.H (1999). Influence of lecithin on some physical, chemical properties of poloxamar gels: Rheological, microscopic and invitro permeation studies, Int. Journal of Pharmaceutics, 193(1):49-55.
Beril T, Andreas D, Rene D.V, Pramod R.S (2002). Bradykinin potentiation by ACE inhibitors: a matter of metabolism, Br. Journal of Pharmacology, 137(2):276-284.
Bernard V.E, Mooter G.V, Patrick A (2008). Top-down production of drug Nanocrystals: Nanosuspension stabilization, miniaturization and transformation into solid products, Int. Journal of Pharmaceutics, 364:264-75.
Bharathi M, Sarat C.P, Lata E.R, Wasim R.S, Ravi T.A, Brito R.S, Bhaskar R.K (2012). Preparation and invitro characterization of Valsartan loaded eudragit Nanoparticles, Der Pharmacia Sinica, 3(5):516-525.
Bhowmik D, Chiranjib B, Jitendra Y, Chandira R.M, Sampath K.P (2010). Emerging trends of disintegrants used in formulation of solid dosage form, Der. Pharmacia Lettre, 2(1): 495-504.
Bindra D.S, Stein D, Pandey P, Barbour N (2014). Incompatibility of crosscarmellose sodium with alkaline excipients in a tablet formulation, Pharm. Dev. Technology, 19(3): 285-289.
Blagden N, Gavan P.T, York P (2007). Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates, Adv. Drug Delivery Review, 59: 617-630.
Bleich J, Muller B.W, Wabmus W (1993). Aerosol solvent extraction system-a new microparticle production technique, Int.. Journal of Pharmaceutics, 97(1):111-117.
Bo H, Thomas J.M, Christine D.K (2008). Nanowire sensors for multiplexed detection of biomolecules, Curr. Opin. Chem. Biology, 12(5):522-528.
Bohm B.H, Muller R.H (1999). Lab scale production unit design for Nanosuspensions of sparingly soluble cytotoxic drugs, Pharm. Sci. Techno. Today, 2:336-339.
Bond L, Allen S, Davies M.C, Roberts C.J, Shivji A.P, Tendler S.J, Williams P.M, Zhang, J (2002). Differential scanning calorimetry and scanning thermal microscopy analysis of pharmaceutical materials, Int. Journal of Pharmaceutics, 243:71-82.
Bourne D.W, Banker G.S, Rhodes C.T (2002). Modern Pharmaceutics, 4th edition, New York, NY, Marcel Dekker Inc,67-92.
Brian W.G, Gina M.G, Lisa L. V.M, David J.G (1998). Analysis of Ritonavir in Plasma/Serum and Tissues by High- performance liquid chromatography, Journal of Pharm. and Toxi. methods, 40:235-239.
Briggs T. L, Maxwell T.J (1973). Process for preparing powder blends, US patent no 3721725.
Brunner E (1904). Reaktionsgeschwindigkeit in heterogenenSystemen, Journal of Phys. Chemistry, 47:56–102.
Buchi N.N, Ramya K.M, Peter A.C (2012). Effect of recrystallization on the pharmaceutical properties of Valsartan for improved therapeutic efficiency, Journal of Applied Pharm. Science, 2(10):126-132.
Published
05/03/2021
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Sudhakar Kancharla, Prachetha Kolli, and Dr.K.Venkata Gopaiah. “Nanosuspension Formulation & Evaluation of Ritonavir & Valsartan by Using Poloxamer As a Stabilizing Agent to Enhance the Oral Bio Availability”. International Journal of Health Care and Biological Sciences, Mar. 2021, pp. 04-17, doi:10.46795/ijhcbs.vi.137.
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