International Journal of Biological Macromolecules 104 (2017) 1229–1237
Contents lists available at ScienceDirect
International Journal of Biological Macromolecules
j ourna l h o mepa ge: www.elsevier.com/locate/ijbiomac
Kondogogu gum-Zn
+2
-pectinate emulgel matrices reinforced with
mesoporous silica for intragastric furbiprofen delivery
Hriday Bera
a,b,∗
, Jhansirani Nadimpalli
b
, Sanoj Kumar
b
, Pavani Vengala
b
a
Faculty of Pharmacy, AIMST University, Semeling, Kedah,08100, Malaysia
b
Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad, 500090, India
a r t i c l e i n f o
Article history:
Received 13 April 2017
Received in revised form 28 May 2017
Accepted 4 July 2017
Available online 5 July 2017
Keywords:
Low methoxyl pectin
Kondogogu gum
Calcium silicate
Emulgel systems
Floatation
Mucoadhesion
a b s t r a c t
Flurbiprofen (FLU), a non-steroidal anti-inflammatory drug, exhibits limited clinical response due to
its poor physicochemical properties. This study aimed at developing reliable drug carriers for intrgas-
tric FLU delivery with a view to improve biopharmaceutical characteristics of drug and modulate its
release in a controlled manner. In this context, FLU-loaded kondogogu gum (KG)-Zn
+2
-low methoxyl
(LM) pectinate emulgel matrices reinforced with calcium silicate (CS) were accomplished by ionotropic
gelation technique employing zinc acetate as cross-linker and characterized for their in vitro perfor-
mances. All the formulations demonstrated excellent drug encapsulation efficiency (DEE, 46–87%) and
sustained drug release behavior (Q
7h
, 70–91%). These quality attributes were remarkably influenced by
polymer-blend (LM pectin:KG) ratios, low-density oil types and CS inclusion. The drug release profile
of the FLU-loaded optimized matrices (F-7) was best fitted in Korsmeyer-Peppas model with Fickian
diffusion driven mechanism. It also conferred excellent in vitro gastroretention capabilities. Moreover,
the drug-excipient compatibility, alteration of crystallinity and thermal behavior of drug and surface
morphology of matrices were evidenced with the results of FTIR, XRD, DSC and SEM analyses, respec-
tively. Thus, the newly developed matrices are appropriate for sustained intragastric FLU delivery and
simultaneous zinc supplementation for effective inflammation and arthritis management.
© 2017 Elsevier B.V. All rights reserved.
1. Introduction
Flurbiprofen (FLU), a non-steroidal anti-inflammatory agent
of 2-arylpropionic acid class, is most widely prescribed drug for
inflammation and arthritis management [1]. It acts by blocking the
action of cyclooxyganase enzyme and eventually controls the pro-
duction of prostaglandins. However, FLU belongs to the BCS class
II and displays poor aqueous solubility. The poor inherent solu-
bility and slow dissolution rate in the gastrointestinal lumen give
rise to extremely variable oral bioavailability and limited clinical
response of FLU. Moreover, it exhibits a shorter half-life (3.9 h)
and produces ulcerogenic adverse effect with abdominal discom-
fort [2]. Hence, there is an unmet need to develop an intelligent
carrier for sustained FLU delivery. An array of scientific investiga-
tions adopted numerous approaches to overcome the challenges
associated with FLU therapy exemplified by FLU-in-cyclodextrin-
in-liposomes [3], FLU-loaded nanostructured lipid carriers based
∗
Corresponding author at: Faculty of Pharmacy, AIMST University, Semeling,
Kedah, 08100, Malaysia.
E-mail address: hriday.bera1@gmail.com (H. Bera).
topical gel [2], FLU-microemulsion [4], FLU-entrapped cross-linked
chitosan microspheres [5] and so on with diverse degrees of
success. In today’s pharmaceutical arena, emulgels, comprising
oil-in-water emulsions within the gel matrices, have emerged as
attractive drug delivery platforms for hydrophobic drugs as they
offer the advantages of both emulsions and gels [6]. Recent investi-
gations have exploited various naturally occurring polysaccharides
such as alginate, pectin, tamarind gum, sterculia gum etc. to accom-
plish stable emulgel systems as drug carriers [7–9].
Kondagogu gum (KG) is a plant-derived substituted rhamno-
galacturonans obtained from Cochlospermum gossypium DC (Family
Bixaceae). KG is composed of arabinose, galactose, rhamnose, glu-
cose, mannose, glucuronic acid and galacturonic acid, with sugar
linkage of (1 → 2) -d-Gal p, (1 → 6) -d-Gal p, (1 → 4) -d-Glc p,
4-O-Me--d-Glc p, (1 → 2) -l-Rha and (1 → 4) -d-Gal p. It dis-
plays outstanding gelling, emulsifying and thickening properties
[10]. Thus, KG could be utilized to fabricate stable emulgels contain-
ing various low-density oils. The oil-entrapped KG based emulgels
could display buoyant property due to their low density. In addi-
tion, the oil phase might impose an effective blockade towards
drug eluting from the matrices, which results in enhanced drug
entrapment with retarded drug release behavior. Therefore, these
http://dx.doi.org/10.1016/j.ijbiomac.2017.07.027
0141-8130/© 2017 Elsevier B.V. All rights reserved.