Tasana Pitaksuteepong

Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets.

The aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various amounts of calcium acetate and then tableting by automatic hydraulic press machine. Differential scanning calorimetry, powder x-ray diffraction, and Fourier transformed-infrared spectroscopy studies of the compressed tablets revealed no drug-polymer interaction and the existence of drug with low crystallinity. The in-vitro release studies in phosphate buffer (United States Pharmacopeia) and tris buffer indicated that the lower the DE, the greater the time for 50% of drug release (T50). This finding is probably because of the increased binding capacity of pectin to calcium. However, when the calcium was excluded, the pectins with different DEs showed similar release pattern with insignificant difference of T50. When the amount of calcium acetate was increased from 0 to 12 mg/tablet, the drug release was significantly slower. However, a large amount of added calcium (ie, 24 mg/tablet) produced greater drug release because of the partial disintegration of tablets. The results were more pronounced in phosphate buffer, where the phosphate ions induced the precipitation of calcium phosphate. In conclusion, both pectin type and added calcium affect the drug release from the pectin-based matrix tablets.

Studies on Pectins as Potential Hydrogel Matrices for Controlled-Release Drug Delivery

Polymeric hydrogels are widely used as controlled-release matrix tablets. In the present study, we investigated high-methoxy pectins for their potential value in controlled-release matrix formulations. The effects of compression force, ratio of drug to pectin, and type of pectin on drug release from matrix tablets were also investigated. The results of the in vitro release studies show that the drug release from compressed matrix tablets prepared from pectin can be modified by changing the amount and the type of pectin in the matrix tablets. However, compression force did not significantly affect the drug release. The mechanisms controlling release rate were discussed with respect to drug diffusion through the polymer matrices, but may be more complex.

Factors influencing the entrapment of hydrophilic compounds in nanocapsules prepared by interfacial polymerisation of water-in-oil microemulsions

This study demonstrates the effect of drug properties and method of loading (sorption and encapsulation) on entrapment within poly(alkyl cyanoacrylate) nanocapsules prepared by interfacial polymerisation of biocompatible water-in-oil microemulsions. For small molecular weight compounds (<1000 Da), entrapment efficiency is more dependent on charge of the compound than on the method used for entrapment. Entrapment efficiency within the negatively charged nanocapsules (zeta potential approximately -30 mV) was in the order cationic compound > neutral compound > anionic compound. Only minimal differences for entrapment efficiency were noted between sorption (addition of the compound 4 h after initiation of the polymerisation) and encapsulation (addition of the compound to microemulsion prior to polymerisation). For high molecular weight compounds, the method used for entrapment however, is very important. For hydrophilic macromolecules such as proteins, high entrapment efficiencies can only be achieved by encapsulation. Entrapment of such compounds seems to be independent of the net charge of the compound being encapsulated but depended on the molecular weight. For nanocapsules prepared by interfacial polymerisation of water-in-oil microemulsions, these findings are useful as a foundation in the development of nanocapsules with desired properties.

Methylated N-(4-N,N-dimethylaminocinnamyl) chitosan-coated electrospray OVA-loaded microparticles for oral vaccination

The purpose of this study was to prepare microparticles entrapping ovalbumin (OVA) as a model antigen to induce immune responses in mice following oral vaccination. In this study, calcium-alginate and calcium-yam-alginate microparticles were prepared by crosslinking alginate with calcium chloride solution using an electrospraying technique. 0.1% (w/v) of methylated N-(4-N,N-dimethylaminocinnamyl) chitosan (TM65CM50CS) was used to coat microparticles entrapping an initial OVA of 20% w/w to polymer. The results indicated that the coated microparticles were spherical and had a smooth surface, with an average size of 1-3 μm, and were positively charged. In addition, the particles demonstrated a greater swelling and mucoadhesive properties than did uncoated microparticles. The in vitro release from the microparticles indicated that the coated microparticles resulted in more sustained release than uncoated microparticles. The cytotoxicity results showed that all of the formulations were safe. The in vivo oral administration demonstrated that at the same amount of 250 μg OVA, coated microparticles exhibited the highest in vivo adjuvant activity in both IgG and IgA immunogenicity.

Entrapment of bioactive molecules in poly (alkylcyanoacrylate) nanoparticles

Poly (alkylcyanoacrylate) [PACA] nanoparticles have been studied since the early 1980s as possible colloidal drug delivery systems. Several excellent general reviews have since been published on this subject. This review focuses on the use of the two different methods (encapsulation and sorption) for the entrapment of drugs and model compounds in PACA nanoparticles. The term encapsulation is used when the drug or model compound is added at the same time or before the monomer to the polymerization template. The term sorption is used when the compound is added after the polymerization has taken place. High drug entrapment can be achieved with both methods and the method of entrapment (encapsulation or sorption) should be chosen depending on the type of drug to be entrapped and the method of particle preparation (interfacial polymerization of a coarse emulsion or a microemulsion or micellar polymerization). The type, chain length, and amount of monomer used for the polymerization as well as possible interactions of the compound with the monomer during polymerization should also be considered in the choice of entrapment method and these can also influence the extent of encapsulation.

Morus alba L. Stem Extract Attenuates Pain and Articular Cartilage Damage in the Anterior Cruciate Ligament Transection-Induced Rat Model of Osteoarthritis

Aim: This study was designed to investigate the anti-nociceptive effect of Morus alba stem extract as well as its cartilage protective effect in the anterior cruciate ligament transection (ACLT)-induced rat model of osteoarthritis (OA). Methods: The anti-nociceptive effect of this plant extract was determined by measuring hind limb weight bearing, while the severity of cartilage damage to the knee joints was evaluated using the modified Mankin grading system. Results: Oral administration of M. alba stem extract (56 and 560 mg/kg) significantly attenuated joint pain as indicated by a significant (p < 0.05) increase in the values of percent weight borne on the operated hind limb for the OA-induced groups that received M. alba stem extract at 56 and 560 mg/kg when compared to those of the vehicle-treated OA-induced group. In addition, a significant improvement in the Mankin score was also observed in rats treated with 560 mg/kg M. alba stem extract, which was in agreement with its pain-relieving effect. Conclusion: The results showed that M. alba stem extract exhibited an anti-nociceptive effect as well as cartilage protection in the ACLT-induced rat model of OA, supporting its potential use as a therapeutic treatment for OA.

In Vitro Anti-Inflammatory Activity of Morus alba L. Stem Extract in LPS-Stimulated RAW 264.7 Cells

Morus alba L., also known as white mulberry or Mhon, has long been used in traditional medicines. This study was aimed to investigate anti-inflammatory activities of mulberry stem ethanolic extract (MSE) in lipopolysaccharide- (LPS-) stimulated RAW 264.7 macrophage cell line. The MSE was first prepared and then investigated for cell viability using the MTT assay. The anti-inflammatory activities were investigated through the inhibition of inducible nitric oxide synthase (iNOS), cyclooxygenase- (COX-) 2 mRNA expression, and iNOS protein expression using reverse transcription-polymerase chain reaction (RT-PCR) assay and immunoblotting analysis, respectively. The inhibition of nitric oxide production of the MSE was also investigated using the Griess reaction assay. The MSE concentration ranging from 10 to 40 µg/ml yielded cell viability higher than 80%. The MSE at concentrations of 20 and 40 µg/ml demonstrated anti-inflammatory activity through the inhibition of nitric oxide production via suppression of both the iNOS mRNA and protein. It was also found to inhibit the expression of COX-2 mRNA in LPS-induced RAW 264.7 cells. This study is the first to report the anti-inflammatory potential of the extract prepared from the stem of mulberry.