NEBIVOLOL HYDROCHLORIDE LOADED NANOSTRUCTURED LIPID CARRIERS AS TRANSDERMAL DELIVERY SYSTEM:-PART 2:- HYDROGEL PREPARATION, EVALUATION AND PERMEATION STUDY

Esraa Ghazy, Alaa Abdulhusain Abdulrasool, Jafar Jaber Al-Tamimi, Nawal Ayash

Abstract


Nebivolol hydrochloride (NEB), is a third generation highly selective β1-blocker, it has an antihypertensive properties. Its elimination half-life is around 10 hrs while its oral bioavailability is about 12%. The objective of the current study was to develop nanostructured lipid carriers (NLCs) for transdermal delivery of (NEB). Through the preparation, characterization and conducting of an in vitro study for (NEB) loaded (NLCs), the formulation of NEB-NLCs based hydrogel using different types of gelling agents was introduced. Moreover, the incorporation of lipid nanoparticles into carbapol 934 as hydrogel base in different formulations was described in this study. The optimized formula (350 mg Glyceryl monostearate, 150 mg oleic acid, 2% (W/W) span 80, and 2% (W/W) Cremophor EL) was tested for entrapment efficiency, particle size and loading capacity then incorporated into hydrogel for expedient transdermal application. A number of measures were implemented for the NEB-NLCs based hydrogel, the results for the optimized formula were found to be as the following: particle size 228 nm, polydispersity index 0.3, zeta potential -29mV, pH 7.05 viscosity 7210cps, spreadability 6 cm, drug content 95%, and Ex Vitro skin permeation 90.8%. The transmission electron microscopy (TEM) and the optical microscope study revealed almost spherical shaped nanoparticles. Nebivolol  based  hydrogel  demonstrated no  skin  irritation  and  showed a  prolong  release  for up  to  24 hrs.  The flux for the permeation study through rat skin was found to be (143μg/cm2/hr). Carbapol 934 was used as a gelling agent; the obtained formula gave evidence for good spreadability, homogeneity and rheological behavior. In conclusion, the data obtained from this study illustrated a successful development of NEB-NLCs-based hydrogel in the increase of the encapsulation efficiency of colloidal lipid carriers. The advantages of the colloidal lipid carriers of the improved performance  were in terms of stability and provides a sustaining NEB transdermal effect.

Keywords: Nebivolol hydrochloride; Nanostructured lipid carriers, Hydrogel, Transdermal delivery


References


- Sovan, L.; Utpal J.; P. K., Manna; G. P., Mohanta, R., Manavalan; Nanoparticle: An overview of preparation and characterization,Journal of Applied Pharmaceutical Science, 2011,l(6): 228-234.

- Sean C.; (BPharm, FRPharmS), Martindale, the complete drug reference, thirty-sixth edition, Pharmaceutical Press 2009, Pp: 1347.

- Anthony, M.; David O.; Brian W.; Clarke's analysis of drugs and poisons, pharmaceutical press 2005:48.

- Budavari S.; The merck index. An encyclopedia of chemicals, drugs and biologicals. edition 3;merck& Co., Inc., whitehouse station, NJ. 200: 1152.

- Deepak, S.; Rajesh, Y.; and Rajesh, A.; Liquid chromatographic method development and validation for assay and dissolution of nebivolol hydrochloride in tablet dosage form, Journal of Chemical and Pharmaceutical Research, 2014; 6(7): 2356-2363.

- Shodhganga, Chapter-5, Determination of nebivolol and its impurities by RP-HPLC method, 2015.

- Ajay, P.; Devendra, S. .; Peeyush. K. and Jhageshwar, V. A review on novel lipid based nanocarriers. review article, inter. J. of phar. and pharm Sci. 2010;2(4).

- Araújo, J.; Gonzalez, E.; Egea, M.; Garcia, M.; Souto E.; Nanomedicines for ocular NSAIDs: safety on drug delivery, nanomedicine, 2009;(5): 394-401.

- Ghazy E.; Abdulrasoo A.; Al-Tamimi J. J.; and Ayash N.; Nebivolol Hydrochloride Loaded Nanostructured Lipid Carriers as Transdermal Delivery System: Part 1: Preparation, Characterization and In Vitro Evaluation. AJPS, 2016;16(1):26-39.

- Manickam B and Shyam SA, Formulation and Evaluation of Chitosan Based Bioadhesive Drug Delivery Systems of Lisinopril for Prolonged Drug Delivery. Pelagia Research Library 2013; 4(3):1-7.

- LavKeshri and Kamla Pathak, Development of thermodynamically stable nanostructured lipid carrier system using central composite design for zero order permeation of Econazole nitrate through epidermis, Pharmaceutical Development and Technology, 2013; 18(3): 634–644.

- Heshu Sulaiman Rahman, Abdullah Rasedee, CheeWun How, et.al; Zerumbone-loaded nanostructured lipid carriers: preparation, characterization, and antileukemic effect, International Journal of Nanomedicine, 2013;(8):2769-2781.

- Jabbar G. E., Formulation and in vitro evaluation of silymarin through rat skin as topical delivery preparation, MSc thesis, College of Pharmacy, University of Baghdad, (2009).

- KumbojiS, DR.Uma MRU, Mahala skhmiK and Shalini KB, Selection of Optimized Transdermal Patch ofAlfuzosin Hydrochloride through Different Approaches. International Journal of Inventions inPharmaceutical Sciences 2013;1(6): 515-525.

- Arfat I, Nisar UR, ZeeshanJ, Muhammad K, Irfan A, Khizar A andTalib H, In Vitro Evaluation of Transdermal Patches of Flurbiprofen With Ethyl Cellulose. ActaPoloniaePharmaceutica-Drug Research 2014; 71(2): 287-295.

- Elton Luiz Silva, GuilhermeCarneiro, Priscila Albuquerque Caetano, et.al., Nanostructured lipid carriers loaded with tributyrin as an alternative to improve anticancer activity of all-trans retinoic acid, Expert Rev. Anticancer Ther.15 (2), 247–256 (2015).

- Yuhui Chen, Lizhen Pan, Ming Jiang, Dong Li, Nanostructured lipid carriers enhance the bioavailability and brain cancer inhibitory efficacy of curcuminbothin vitro and in vivo, 2015 Informa Healthcare USA.

- Müller RH, Petersen RD, Hommoss A, Pardeike J. Nanostructured lipid carriers (NLC) in cosmetic dermal products. Adv Drug Deliv Rev. 2007;59:522–530.13. de Jong EMGJ, M.

- Chen H, Chang X, Du D, et al. Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting. J Control Release. 2006;110:296–306.

- Lombardi Borgia S, Regehly M, Sivaramakrishnan R, et al. Lipid nanoparticles for skin penetration enhancement – correlation to drug localization within the particle matrix as determined by fluorescence and parelectric spectroscopy. J Control Release. 2005;110:151–163.

- Robert A. turner, Screening method in pharmacology, Academic press,New York and London,(1965).


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