WATER UPTAKE PERFORMANCE OF BIOADHESIVE HPMC MICROPARTICLES FOR NASAL ADMINISTRATION USING DIFFERENT PROCESSING VARIABLES OF CO-PRECIPITATION TECHNIQUE

Authors

  • Issraa Rasheed Abed Al-rahman Al-Obaidi Pharmaceutics Department, College of Pharmacy, University of Baghdad
  • Issam Yasser Husean Ministry of Health, Baghdad, Iraq.

Keywords:

Bioadhesive microparticles, Water sorption, Nasal drug delivery, Dynamic adhesion, Co-precipitation technique, HPMC polymer, Differential scanning calorimetry

Abstract

Objective: An aqueous-organic precipitation technique was developed for preparing bioadhesive hydroxypropyl methylcellulose (HPMC) microparticles for nasal delivery using a low viscosity grade of HPMC K100LV.

Methods: The method involved the preparation of HPMC microparticles by precipitating the gelled HPMC into acetone. The effect of different processing variables of precipitation technique on in-vitro bioadhesive performance of HPMC microparticles was studied.

Results: In-vitro assessment of adhesion properties of the microparticles showed that the process of co-precipitation greatly increased the adhesiveness in comparison with unprocessed HPMC powder. Bioadhesive performance was found to be dependent on the dehydrated state of the polymer following precipitation, with the most dehydrated formulations using the slowest (dropwise) rate of addition of the HPMC gel to acetone, showing lower water uptake and greater adhesive performance. It would be expected therefore, that the interaction of acetone and water would be instantaneous and complete, resulting in an extremely efficient dehydration process and a collapse of HPMC matrix structure, forming a physical barrier to subsequent rehydration.

Conclusion: This formulation afforded the highest bioadhesion score in the test employed, which was designed to represent the dynamic interplay of hydration, entanglement of polymer and mucin, and rheological flow which a formulation would experience on the nasal mucosal surface.

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References

Lansley AB, Martin GP: Nasal drug delivery. in Hillery AM, Lloyd AW, Swarbrick J (eds): Drug Delivery and Targeting for Pharmacists and Pharmaceutical Scientists. London: Taylor & Francis, 2001, p.215-43.

Corbo GM, Foresi A, Bonfitto P, Mugnano A, Agabiti N, Cole PJ. Measurement of nasal mucociliary clearance. Arch Dis Child 1989;64:546-50.

Stanley PJ, Wilson R, Greenstone MA, MacWilliam L, Cole PJ. Effect of cigarette smoking on nasal mucociliary clearance and ciliary beat frequency. Thorax 1986;41:519-23.

Lee JW, Park JH, Robinson JR. Bioadhesive-based dosage forms:the next generation. J Pharm Sci 2000;89:850-66.

Nakamura K, Maitani Y, Lowman AM, Takayama K, Peppas NA, Nagai T. Uptake and release of budesonide from mucoadhesive, pH-sensitive copolymers and their application to nasal delivery. Journal of controlled release:official journal of the Controlled Release Society 1999;61:329-35.

McInnes FJ, O'Mahony B, Lindsay B, Band J, Wilson CG, Hodges LA, Stevens HN: Nasal residence of insulin containing lyophilised nasal insert formulations, using gamma scintigraphy. Eur J Pharm Sci 2007;31:25-31.

Mortazavi AS, Smart JD, J. An investigation into the role of water movement and mucus gel dehydration in mucoadhesion. J Control Release 1993;25:197-203.

Smart JD, Kellaway IW, Worthington HE. An in-vitro investigation of mucosa-adhesive materials for use in controlled drug delivery. J Pharm Pharmacol 1984;36(5):295-9.

Andrews GP, Laverty TP, Jones DS. Mucoadhesive polymeric platforms for controlled drug delivery. Eur J Pharm Biopharm 2009;71(3):505-18.

Dyvik K, Graffner C. Investigation of the applicability of a tensile testing machine for measuring mucoadhesive strength. Acta Pharm Nord 1992;4(2):79-84.

Jadhav KR, Gambhire MN, Shaikh IM, Kadam VJ, Pisal SS. Nasal drug delivery system-factors affecting and applications. Cur Drug Therapy 2007;2:27-38.

McInnes F, Thapa P, Stevens HNE, Baillie AJ, Watson DG, Nolan A, Gibson I: Nasal absorption of nicotine in sheep from a lyophilised insert formulation. In AAPS Conference. US, AAPS PharmSci, 2000.

Pennington AK, Ratcliffe JH, Wilson CG, Hardy JG, J. The influence of solution viscosity on nasal spray deposition and clearance. Int J Pharm 1988;43:221-4.

Furubayashi T, Inoue D, Kamaguchi A, Higashi Y, Sakane T. Influence of formulation viscosity on drug absorption following nasal application in rats. Drug Metab Pharmacokinet 2007;22(3):206-11.

Zaki NM, Awad GAS, Mortada ND, Abd ElHady SS. Rapid-onset intranasal delivery of metoclopramide hydrochloride. Part I. Influence of formulation variables on drug absorption in anesthetized rats. Int J Pharm 2006;327(1-2):89-96.

McInnes F, Baillie AJ, Stevens HNE. The use of simple dynamic mucosal models and confocal microscopy for the evaluation of lyophilised nasal formulations. J Pharm Pharmacol 2007;59(6):759-67.

Chaturvedi M, Kumar M, Pathak K. A review on mucoadhesive polymer used in nasal drug delivery system. J Adv Pharm Technol Res 2011;2(4):215-22.

Hou Q, Chau DY, Pratoomsoot C, Tighe PJ, Dua HS, Shakesheff KM, Rose FR: In situ gelling hydrogels incorporating microparticles as drug delivery carriers for regenerative medicine. J Pharm Sci 2008;97:3972-80.

Siepmann J, Siepmann F. Microparticles used as drug delivery systems. Prog Colloid Polym Sci 2006;133:15-21.

De Ascentiis A, Bettini R, Caponetti G, Catellani PL, Peracchia MT, Santi P, Colombo P: Delivery of nasal powders of beta-cyclodextrin by insufflation. Pharm Res 1996;13:734-8.

Wermeling DP, Miller JL: Intranasal drug delivery. in Rathbone MJ, Hadgraft J, Roberts MS (eds): Modified-Release Drug Delivery Technology. New York: M. Dekker, 2003, p.727-48.

Dandge HB, Dehghan MHG, J. Formulation and evaluation of nasal mucoadhesive microparticles of diltiazem hydrochloride. Int J Chem Tech Res 2009;1:1036-42.

Harikarnpakdee S, Lipipun V, Sutanthavibul N, Ritthidej GC. Spray-dried mucoadhesive microspheres:preparation and transport through nasal cell monolayer. AAPS PharmSciTech 2006;7(1):E12.

Hascicek C, Gonul N, Erk N. Mucoadhesive microspheres containing gentamicin sulfate for nasal administration: preparation and in vitro characterization. Farmaco 2003;58:11-6.

Lim ST, Forbes B, Martin GP, Brown MB. In vivo and in vitro characterization of novel microparticulates based on hyaluronan and chitosan hydroglutamate. AAPS PharmSciTech 2001;2(4):20.

Lim ST, Martin GP, Berry DJ, Brown MB. Preparation and evaluation of the in vitro drug release properties and mucoadhesion of novel microspheres of hyaluronic acid and chitosan. J Control Release 2000;66(2-3):281-92.

Swamy NGN, Abbas Z. Preparation and in vitro characterization of mucoadhesive hydroxypropyl guar microspheres containing amlodipine besylate for nasal administration. Indian J Pharm Sci 2011;73(6):608-14.

Ramteke KH, Jadhav VB, Dhole SN: Microspheres: as carriers used for novel drug delivery system IOSRPHR 2012;2:44-8.

Swamy NG, Abbas Z. Preparation and in vitro characterization of mucoadhesive polyvinyl alcohol microspheres containing amlodipine besylate for nasal administration. IJPER 2012;46:52-8.

Yeo Y, Baek N, Park K. Microencapsulation methods for delivery of protein drugs. Biotechnol Bioprocess Eng 2001;6:213-30.

Rowe RC, Sheskey PJ, Weller PJ: Hypromellose. in Rowe RC, Sheskey PJ, Weller PJ (eds): Handbook of Pharmaceutical Excipients London: Pharmaceutical Press and American Pharmaceutical Association, 2003, p.326-29.

Yamashita K, Nakate T, Okimoto K, Ohike A, Tokunaga Y, Ibuki R, Higaki K, Kimura T: Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm 2003;267:79-91..

Bertram U, Bodmeier R. In situ gelling, bioadhesive nasal inserts for extended drug delivery:in vitro characterization of a new nasal dosage form. Eur J Pharm Biopharm 2006;27(1):62-71.

McInnes F, Baillie AJ, Stevens HNE: Quantification of adhesion of lyophilised HPMC formulations using a novel dynamic adhesion test. In AAPS Conference. US, AAPS Pharm Sci, 2001.

Okhamafe AO, York P. Interaction Phenomena in some Aqueous-Based Tablet Coating Polymer Systems. Pharm Res 1985;2(1):19-23.

Shukla SK. Study of solvent-solvent interaction by paper chromatography II. Acetone water system Chromatographia 1973;6:463-7.

Katzhendler I, Mäder K, Friedman M. Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. Int J Pharm 2000;200(2):161-79.

Bruni G, Milanese C, Bellazzi G, Berbenni V, Cofrancesco P, Marini A, Villa M: Quantification of drug amorphous fraction by DSC. J Therm Anal Cal 2007;89:761–6.

Laksmana FL, Kok PJAH, Frijlink HW, Vromans H, Van der Voort Maarschalk K. Using the internal stress concept to assess the importance of moisture sorption-induced swelling on the moisture transport through the glassy HPMC films. AAPS PharmSciTech 2008;9(3):891-8.

Anuar NK, Wui WT, Ghodgaonkar DK, Taib MN. Characterization of hydroxypropylmethylcellulose films using microwave non-destructive testing technique. J Pharm Biomed Anal 2007;43(2):549-57.

Alur HH, Pather SI, Mitra AK, Johnston TP. Transmucosal sustained-delivery of chlorpheniramine maleate in rabbits using a novel, natural mucoadhesive gum as an excipient in buccal tablets. Int J Pharm 1999;188(1):1-10.

Alfadhel M, Puapermpoonsiri U, Ford SJ, McInnes FJ, van der Walle CF. Lyophilized inserts for nasal administration harboring bacteriophage selective for Staphylococcus aureus:in vitro evaluation. Int J Pharm 2011;416(1):280-7.

McInnes FJ, Thapa P, Baillie AJ, Welling PG, Watson DG, Gibson I, Nolan A, Stevens HN: In vivo evaluation of nicotine lyophilised nasal insert in sheep. Int J Pharm 2005;304:72-82.

Holzgrabe U, Wawer I, Diehl B: MR Imaging and MR Spectroscopy. in Wawer I (ed): NMR spectroscopy in drug development and analysis. Weinheim; Chichester: Wiley-VCH, 1999, p.257-86..

Aloorkar NH, Bhatia MS. Synthesis, characterization and evaluation of effect of chemical modification of hydroxypropyl methylcellulose on drug release. Der Pharmacia Lettre 2010;2(4):509-19.

Gilard P, Pope C, Bore P: Appendix: Spectral Libraries in Bore P (ed): Cosmetic analysis: selective methods and techniques. New York: Marcel Dekker INC, 1985, p.436-7.

Published

01-07-2014

How to Cite

Al-Obaidi, I. R. A. A.- rahman, and I. Y. Husean. “WATER UPTAKE PERFORMANCE OF BIOADHESIVE HPMC MICROPARTICLES FOR NASAL ADMINISTRATION USING DIFFERENT PROCESSING VARIABLES OF CO-PRECIPITATION TECHNIQUE”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 6, no. 7, July 2014, pp. 225-31, https://journals.innovareacademics.in/index.php/ijpps/article/view/1736.

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