Effect of solvent on properties of pectin microspheres prepared by emulsion-dehydration technique

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aDepartment of Pharmaceutical Technology,Faculty of Pharmacy,Silpakorn University,Nakhon Pathom 73000, Thailand

bPharmaceutical Biopolymer Group(PBiG),Faculty of Pharmacy,Silpakorn University,Nakhon Pathom 73000, Thailand

Effect of solvent on properties of pectin microspheres prepared by emulsion-dehydration technique

Tassanee Nernploda,b,Pornsak Sriamornsaka,b,*

aDepartment of Pharmaceutical Technology,Faculty of Pharmacy,Silpakorn University,Nakhon Pathom 73000, Thailand

bPharmaceutical Biopolymer Group(PBiG),Faculty of Pharmacy,Silpakorn University,Nakhon Pathom 73000, Thailand

A R T I C L E I N F O

Article history:

Available online 25 November 2015

Theophylline

Pectin microspheres

Emulsion-dehydration technique

In the controlled release area,biodegradable microspheres are one of the most helpful devices to deliver materials in an effective,prolonged and safe manner[1].Biodegradable pectin microspheres could provide an approach for developing controlled release drug delivery systems.Pectin is a naturally occurring,non-toxic,water-soluble polysaccharide used in many food industries.Pectin has increasingly gained acceptance as a carrier polymer for site-specifc delivery and controlled release dosage forms,such as beads,pellets,tablets,and flms[1,2]. The purpose of this study was to prepare pectin microspheres containing theophylline by emulsion-dehydration technique. The effect of solvent used for dehydration on properties of pectin microspheres was also studied.

To prepare theophylline-loaded pectin microspheres by emulsion-dehydration technique,isooctane containing 1.25% (w/v)Span®83 was used as internal phase in water-in-oil(w/o) emulsions.Various solvents(i.e.,isopropyl alcohol(IPA),absolute ethanol(EtOH)and acetone)were used to dehydrate the pectin microspheres.The pectin microspheres were fltered and dried with freeze dryer.The obtained pectin microspheres were characterized by scanning electron microscopy(SEM),differential scanning calorimetry(DSC),powder X-ray diffractometry (PXRD)and in vitro release study.The morphology of the ophylline-loaded pectin microspheres dehydrated by different solvents demonstrated pectin microspheres with different shapes.Using EtOH demonstrated theophylline crystals on the surface of microspheres while the agglomeration of spherical pectin microspheres was observed when using IPA as dehydrating solvent.The pectin microspheres dehydrated by acetone were irregular in shape.From the DSC thermograms, theophylline-loaded pectin microspheres showed no endothermic melting peak of theophylline suggesting a completed incorporation of theophylline in pectin microspheres,except that using EtOH as dehydrating solvent.The results of PXRD confrmed that there was no crystalline peak in the case of pectin microspheres using IPA and acetone as dehydrating solvent.A burst release in the frst 15 minutes was observed in all pectin microspheres resulting from the rapid release ofdrug from the microspheres and of pectin microspheres themselves.The release of theophylline from pectin microspheres dehydrated by IPA was higher than that by EtOH and acetone, respectively.From the observed results,it is seen that theophylline-loaded pectin microspheres prepared by emulsiondehydration technique could not prolong the drug release. Therefore,the modifcation of microsphere preparation is required to prolong the drug release from pectin microspheres.

Fig.1–SEM photographs of pectin microspheres dehydrated by EtOH(A),IPA(B)and acetone(C),and drug release profle (D).

R E F E R E N C E S

[1]Dashoa A,Jain CP.Development and characterization of pectin-prednisolone microspheres for colon targeted delivery. Int J Chem Tech Res 2009;1:751–757.

[2]Sriamornsak P,Prakongpan S,Puttipipatkhachorn S,et al. Development of sustained release theophylline pellets coated with calcium pectinate.J Control Release 1997;47:221–232.

*E-mail address:sriamornsak_p@su.ac.th.

Peer review under responsibility of Shenyang Pharmaceutical University.

http://dx.doi.org/10.1016/j.ajps.2015.11.028

1818-0876/©2016 Production and hosting by Elsevier B.V.on behalf of Shenyang Pharmaceutical University.This is an open access article under the CC BY-NC-ND license(http://creativecommons.org/licenses/by-nc-nd/4.0/).