Formulation and Pharmacokinetic Evaluation of Phosal Based Zaltoprofen Solid Self-Nanoemulsifying Drug Delivery System

Author(s): Rajan Kalamkar*, Shailesh Wadher.

Journal Name: Pharmaceutical Nanotechnology

Volume 7 , Issue 4 , 2019

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Graphical Abstract:


Abstract:

Background: Phosal based excipients are liquid concentrates containing phospholipids. They are used to solubilize water-insoluble drug and also act as an emulsifier to get the smallest droplet size of the formed emulsion after administration.

Objective: The aim is to prepare phosal based self nanoemulsifying drug delivery system (SNEDDS) for water insoluble drug zaltoprofen.

Methods: The various parameters like solubility of drug in different vehicles, ternary phase diagram are considered to formulate the stable emulsion which is further characterized by Self emulsification time and globule size analysis to optimize liquid SNEDDS of Zaltoprofen. Optimized L-SNEDDS was converted into free-flowing powder Solid-SNEDDS (S-SNEDDS). S-SNEDDS was evaluated for Globule size analysis after reconstitution, in vitro dissolution study and in vivo pharmacokinetic study in rats.

Results: Phosal 53 MCT with highest drug solubility was used as oil along with Tween 80 and PEG 400 as surfactant and cosurfactant respectively to prepare liquid SNEDDS. Neusilin us2 was used as an adsorbent to get free-flowing S-SNEDDS. S-SNEDDS showed improved dissolution profile of the drug as compared to pure drug. In vivo study demonstrated that there is a significant increase in Cmax and AUC of S-SNEDDS compared to zaltoprofen powder.

Conclusion: Phosal based SNEDDS formation can be successfully used to improve the dissolution and oral bioavailability of poorly soluble drug zaltoprofen.

Keywords: Dissolution, pharmacokinetic, phosal, self nanoemulsifying drug delivery system, solubility, zaltoprofen.

[1]
Balakumar K, Habibur Rahman SM, Tamil SN, et al. Design, formulation, in vitro, in vivo, and pharmacokinetic evaluation of Nisoldipine-loaded self-nano-emulsifying drug delivery system. J Nanopart Res 2015; 17: 34.
[2]
Kawabata Y, Wada K, Nakatani M, Yamada S, Onoue S. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications. Int J Pharm 2011; 420(1): 1-10.
[3]
Desai VakaS, Nanvit H, Jain A, Phuapradit W. Self- Nanoemulsion of Poorly Soluble Drugs United States Patent 9511078B26,. 2016.
[4]
Kang BK, Lee JS, Chon SK, et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm 2004; 274(1-2): 65-73.
[5]
Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of self-microemulsifying drug delivery system of oridonin. Int J Pharm 2008; 355(1-2): 269-76.
[6]
Setthacheewakul S, Mahattanadul S, Phadoongsombut N, Pichayakorn W, Wiwattanapatapee R. Development and evaluation of self-microemulsifying liquid and pellet formulations of curcumin, and absorption studies in rats. Eur J Pharm Biopharm 2010; 76(3): 475-85.
[7]
Date AA, Desai N, Dixit R, Nagarsenker M. Self-nanoemulsifying drug delivery systems: formulation insights, applications and advances. Nanomedicine 2010; 5(10): 1595-616.
[8]
Singh B, Bandopadhyay S, Kapil R, Singh R, Katare O. Self-emulsifying drug delivery systems (SEDDS): formulation development, characterization, and applications. Crit Rev Ther Drug Carrier Syst 2009; 26(5): 427-521.
[9]
Kohli K, Chopra S, Dhar D, Arora S, Khar RK. Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability. Drug Discov Today 2010; 15(21-22): 958-65.
[10]
Van Hoogevest P. Review - An update on the use of oral phospholipid excipients. Eur J Pharm Sci 2017; 108: 1-12.
[11]
Ito A, Mori Y. Effect of a novel anti-inflammatory drug, 2-(10, 11-dihydro-10-oxo-dibenzo[b,f]-thiepin-2-yl)propionic acid (CN-100), on the proteoglycan biosynthesis in articular chondrocytes and prostaglandin E2 production in synovial fibroblasts. Res Commun Chem Pathol Pharmacol 1990; 70(2): 131-42.
[12]
Ministry of health, labour and welfare.Japanese Pharmacopoeia. Tokyo: Ministry of health, labour and welfare 2011.
[13]
Chatap V, Marathe G, Maurya A. Formulation and evaluation of zaltoprofen fast disintegrating tablet. J Pharm Sci Technol 2013; 3(1): 20.
[14]
Baek JS, Lim JH, Kang JS, Shin SC, Jung SH, Cho CW. Enhanced transdermal drug delivery of zaltoprofen using a novel formulation. Int J Pharm 2013; 453(2): 358-62.
[15]
Desai NS, Nagarsenker MS. Design and evaluation of self-nanoemulsifying pellets of repaglinide. AAPS PharmSciTech 2013; 14(3): 994-1003.
[16]
Balakrishnan P, Lee BJ, Oh DH, et al. Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS). Eur J Pharm Biopharm 2009; 72(3): 539-45.
[17]
Patel HK, Patel PV, Misan CK, Mehta DS, Patel MB. Development and characterization of liquid and solid selfmicroemulsifying drug delivery system of Tacrolimus. Asian J Pharm 2012; 6: 204-11.
[18]
Agrawal AG, Kumar A, Gide PS. Self-emulsifying drug delivery system for enhanced solubility and dissolution of glipizide. Colloids Surf B Biointerfaces 2015; 126: 553-60.
[19]
Bakhle SS, Avari JG. Development and characterization of solid self-emulsifying drug delivery system of cilnidipine. Chem Pharm Bull 2015; 63(6): 408-17.
[20]
Barakat NS. Enhanced oral bioavailability of etodolac by self-emulsifying systems: in-vitro and in-vivo evaluation. J Pharm Pharmacol 2010; 62(2): 173-80.
[21]
Manish Kumar T, Srikanth G, Pamulaparthya V, Rao JV. Development and validation of HPLC-UV method for the estimation of zaltoprofen in human plasma. J Pharm Res 2011; 4(10): 3753-5.
[22]
Hari Krishna E, Gupta VR, Jyothi S. Comparative pharmacokinetics of prepared zaltoprofen spherical agglomerated dense compacts with commercial product. Int J Pharm Sci Rev Res 2013; 18(1): 165-9.
[23]
Yang HK, Kim SY, Kim JS, Sah H, Lee HJ. Application of column-switching HPLC method in evaluating pharmacokinetic parameters of zaltoprofen and its salt. Biomed Chromatogr 2009; 23(5): 537-42.
[24]
Fahmy UA, Ahmed OA, Hosny KM. Development and evaluation of avanafil self-nanoemulsifying drug delivery system with rapid onset of action and enhanced bioavailability. AAPS PharmSciTech 2015; 16(1): 53-8.
[25]
Qian J, Meng H, Xin L, et al. Self-nanoemulsifying drug delivery systems of myricetin: formulation development, characterization, and in vitro and in vivo evaluation. Colloids Surf B Biointerfaces 2017; 160: 101-9.
[26]
Pornsak S, Sontaya L, Suchada P, Punyanutch M, Zongkang H. A new self-emulsifying formulation of mefenamic acid with enhanced drug dissolution. Asian J Pharm Sci 2015; 10: 121-7.
[27]
Nazari-Vanani R, Moezi L, Heli H. In vivo evaluation of a self-nanoemulsifying drug delivery system for curcumin. Biomed Pharmacother 2017; 88: 715-20.
[28]
Inugala S, Eedara BB, Sunkavalli S, et al. Solid self-nanoemulsifying drug delivery system (S-SNEDDS) of darunavir for improved dissolution and oral bioavailability: In vitro and in vivo evaluation. Eur J Pharm Sci 2015; 74: 1-10.
[29]
Huo T, Tao C, Zhang M, et al. Preparation and comparison of tacrolimus-loaded solid dispersion and self-microemulsifying drug delivery system by in vitro/in vivo evaluation. Eur J Pharm Sci 2018; 114: 74-83.
[30]
Tung NT, Tran CS, Pham TM, et al. Development of solidified self-microemulsifying drug delivery systems containing l-tetrahydropalmatine: design of experiment approach and bioavailability comparison. Int J Pharm 2018; 537(1-2): 9-21.


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Article Details

VOLUME: 7
ISSUE: 4
Year: 2019
Page: [328 - 338]
Pages: 11
DOI: 10.2174/2211738507666190802141754

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