Abstract: The aim of the present study was to evaluate the
mucoadhesion and the release of nicotinamide gel formulations using
in vitro methods. An agar plate technique was used to investigate the
adhesiveness of the gels whereas a diffusion apparatus was employed
to determine the release of nicotinamide from the gels. In this
respect, 10% w/w nicotinamide gels containing bioadhesive
polymers: Carbopol 934P (0.5-2% w/w), hydroxypropylmethyl
cellulose (HPMC) (4-10% w/w), sodium carboxymethyl cellulose
(SCMC) (4-6% w/w) and methylcellulose 4000 (MC) (3-5% w/w)
were prepared. The gel formulations had pH values in the range of
7.14 - 8.17, which were considered appropriate to oral mucosa
application. In general, the rank order of pH values appeared to be
SCMC > MC4000 > HPMC > Carbopol 934P. Types and
concentrations of polymers used somewhat affected the
adhesiveness. It was found that anionic polymers (Carbopol 934 and
SCMC) adhered more firmly to the agar plate than the neutral
polymers (HPMC and MC 4000). The formulation containing 0.5%
Carbopol 934P (F1) showed the highest release rate. With the
exception of the formulation F1, the neutral polymers tended to give
higher relate rates than the anionic polymers. For oral tissue
treatment, the optimum has to be balanced between the residence
time (adhesiveness) of the formulations and the release rate of the
drug. The formulations containing the anionic polymers: Carbopol
934P or SCMC possessed suitable physical properties (appearance,
pH and viscosity). In addition, for anionic polymer formulations,
justifiable mucoadhesive properties and reasonable release rates of
nicotinamide were achieved. Accordingly, these gel formulations
may be applied for the treatment of oral mucosal lesions.
Abstract: In the present study, development of salbutamol
sulphate nanoparticles that adhere to gastric mucus was investigated.
Salbutamol sulphate has low bioavailability due to short transit time in
gastric. It also has a positive surface charge that provides hurdles to be
encapsulated by the positively strong mucoadhesive polymer of
chitosan. To overcome the difficulties, the surface charge of active
ingredient was modified using several nonionic and anionic
stomach-specific polymers. The nanoparticles were prepared using
ionotropic gelation technique. The evaluation involved determination
of particle size, zeta potential, entrapment efficiency, in vitro drug
release and in vitro mucoadhesion test. Results exhibited that the use
of anionic alginate polymer was more satisfactory than that of
nonionic polymer. Characteristics of the particles was nano-size, high
encapsulation efficiency, fulfilled the drug release requirements and
adhesive towards stomach for around 11 hours. This result shows that
the salbutamol sulphate nanoparticles can be utilized for improvement
its delivery.
Abstract: Chitosan is a biopolymer composed of glucosamine
and N-acetyl glucosamine. Solubility and viscosity pose problems in
some applications. These problems can be overcome with unique
modifications. In this study, firstly, chitosan was modified by caffeic
acid and thioglycolic acid, separately. Then, growing effects of these
modified polymers was observed in U937 cell line. Caffeic acid is a
phenolic compound and its modifications act carcinogenic inhibitors
in drugs. Thiolated chitosans are commonly being used for drugdelivery
systems in various routes, because of enhancing
mucoadhesiveness property. U937 cell line was used model cell for
leukaemia. Modifications were achieved by 1 – 15 % binding range.
Increasing binding ratios showed higher radical-scavenging activity
and reducing cell growth, in compared to native chitosan. Caffeic
acid modifications showed higher radical-scavenging activity than
thiolated chitosans at the same concentrations. Caffeic acid and
thioglycolic acid modifications inhibited growth of U937, effectively.