Enteric coating of granules containing the probiotic Lactobacillus acidophilus

In the present study, a capsule formulation composed of enteric coated granules of Lactobacillus acidophilus ATCC 4962 was developed using Eudragit L30D-55 as enteric polymer. Optimization of the capsule formulation was achieved with a maximum viable cell count after 2 h of incubation in acid medium and disintegration time of 1 h in buffer pH 6.8. The amount of Eudragit L30D-55 in the capsules correlated with gastric juice resistance. The best protective qualities against artificial gastric juice were observed when capsules were prepared from granules composed of L. acidophilus, corn starch, lactose monohydrate, polyvinylpyrrolidone and coated with 12.5 % (m/V) of Eudragit L30D-55. Capsule formulation of L. acidophilus in edible broth medium suspension serves as a cheap alternative to the expensive freeze-drying procedure for preparing L. acidophilus. In addition, the enteric coating using Eudragit L30D-55 could protect probiotics from the acidic gastric environment and enhance the bioactivity of probiotics along with replacement of pathogenic microbes in human intestine

Development, Characterisation And Release Study Of Encapsulated Curcumin Microparticles.

Curcumin, the major yellow pigment of Curcuma longa L., has been traditionally used to treat inflammation, skin wounds and tumors. The major disadvantage of curcumin is its high colour intensity, which stains fabrics when in contact with the treated skin

Characterisation of Physicochemical Properties of Propionylated Corn Starch and Its Application as Stabiliser

A series of propionylated starches with diff erent degrees of substitution (DS) was synthesised and their physicochemical properties and application as a stabiliser were investigated. Starch propionates with moderate DS were prepared by esterifi cation of native corn starch with propionic anhydride. By varying the reaction times of the esterifi cation process, twelve starch propionates with DS of 0.47 to 0.94 were prepared. FTIR and NMR confi rmed the introduction of propionyl groups to the starch. X-ray diff raction patt ern showed reduced crystallinity in the starch propionates. The contact angle was found to increase proportionately with the increase in DS. Swelling power results showed that starch propionates were able to swell more than native corn starch at low temperature (40 °C). Oil-in- -water (O/W) emulsions prepared using starch propionates (DS of 0.64 to 0.86) showed exceptional stability when challenged by centrifugation stress test. These stable O/W emulsions had viscosities in the range of 1236.7–3330.0 mPa·s. In conclusion, moderately substituted short-chain (propionylated) starches could be a promising cold swelling starch, thickener and O/W emulsion stabiliser in food, pharmaceutical and cosmetic industries

Solubilization of beclomethasone dipropionate in sterically stabilized phospholipid nanomicelles (SSMs): physicochemical and in vitro evaluations

Mohanad Naji Sahib, Shaymaa Abdalwahed Abdulameer, Yusrida Darwis, Kok Khiang Peh, Yvonne Tze Fung TanSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, MalaysiaBackground: The local treatment of lung disorders such as asthma and chronic obstructive pulmonary disease via pulmonary drug delivery offers many advantages over oral or intravenous routes of administration. This is because direct deposition of a drug at the diseased site increases local drug concentrations, which improves the pulmonary receptor occupancy and reduces the overall dose required, therefore reducing the side effects that result from high drug doses. From a clinical point of view, although jet nebulizers have been used for aerosol delivery of water-soluble compounds and micronized suspensions, their use with hydrophobic drugs has been inadequate.Aim: To evaluate the feasibility of sterically stabilized phospholipid nanomicelles (SSMs) loaded with beclomethasone dipropionate (BDP) as a carrier for pulmonary delivery.Methods: 1,2-Distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 5000) polymeric micelles containing BDP (BDP-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and in vitro characteristics of BDP-SSMs were investigated.Results: BDP-SSMs were successfully prepared with a content uniformity and reproducibility suitable for pulmonary administration. The maximum solubility of BDP in SSMs was approximately 1300 times its actual solubility. The particle size and zeta potential of BDP-SSMs were 19.89 ± 0.67 nm and -28.03 ± 2.05 mV, respectively. The SSMs system slowed down the release of BDP and all of the aerodynamic values of the aerosolized rehydrated BDP-SSMs were not only acceptable but indicated a significant level of deposition in the lungs.Conclusion: The SSM system might be an effective way of improving the therapeutic index of nebulized, poorly soluble corticosteroids.Keywords: beclomethasone, PEGylated polymer, aerodynamic, in vitro dissolutio

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Mohanad Naji Sahib, Yusrida Darwis, Kok Khiang Peh, Shaymaa Abdalwahed Abdulameer, Yvonne Tze Fung TanSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, MalaysiaBackground: Inhaled corticosteroids provide unique systems for local treatment of asthma or chronic obstructive pulmonary disease. However, the use of poorly soluble drugs for nebulization has been inadequate, and many patients rely on large doses to achieve optimal control of their disease. Theoretically, nanotechnology with a sustained-release formulation may provide a favorable therapeutic index. The aim of this study was to determine the feasibility of using sterically stabilized phospholipid nanomicelles of budesonide for pulmonary delivery via nebulization.Methods: PEG5000-DSPE polymeric micelles containing budesonide (BUD-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and pharmacodynamic characteristics of BUD-SSMs were investigated.Results: The optimal concentration of solubilized budesonide at 5 mM PEG5000-DSPE was 605.71 ± 6.38 µg/mL, with a single-sized peak population determined by photon correlation spectroscopy and a particle size distribution of 21.51 ± 1.5 nm. The zeta potential of BUD-SSMs was -28.43 ± 1.98 mV. The percent entrapment efficiency, percent yield, and percent drug loading of the lyophilized formulations were 100.13% ± 1.09%, 97.98% ± 1.95%, and 2.01% ± 0.02%, respectively. Budesonide was found to be amorphous by differential scanning calorimetry, and had no chemical interaction with PEGylated polymer according to Fourier transform infrared spectroscopy. Transmission electron microscopic images of BUD-SSMs revealed spherical nanoparticles. BUD-SSMs exhibited prolonged dissolution behavior compared with Pulmicort Respules® (P , 0.05). Aerodynamic characteristics indicated significantly higher deposition in the lungs compared with Pulmicort Respules®. The mass median aerodynamic, geometric standard deviation, percent emitted dose, and the fine particle fraction were 2.83 ± 0.08 µm, 2.33 ± 0.04 µm, 59.13% ± 0.19%, and 52.31% ± 0.25%, respectively. Intratracheal administration of BUD-SSMs 23 hours before challenge (1 mg/kg) in an asthmatic/chronic obstructive pulmonary disease rat model led to a significant reduction in inflammatory cell counts (76.94 ± 5.11) in bronchoalveolar lavage fluid compared with administration of Pulmicort Respules® (25.06 ± 6.91).Conclusion: The BUD-SSMs system might be advantageous for asthma or chronic obstructive pulmonary disease and other inflammatory airway diseases.Keywords: micelles, PEGylated polymer, aerodynamics, pharmacodynamic

Fizikalno-kemijska svojstva hidroksipropiliranog kukuruznog škroba te njegova moguća primjena kao stabilizatora emulzija

A series of propionylated starches with diff erent degrees of substitution (DS) was synthesised and their physicochemical properties and application as a stabiliser were investigated. Starch propionates with moderate DS were prepared by esterifi cation of native corn starch with propionic anhydride. By varying the reaction times of the esterification process, twelve starch propionates with DS of 0.47 to 0.94 were prepared. FTIR and NMR confirmed the introduction of propionyl groups to the starch. X-ray diffraction pattern showed reduced crystallinity in the starch propionates. The contact angle was found to increase proportionately with the increase in DS. Swelling power results showed that starch propionates were able to swell more than native corn starch at low temperature (40°C). Oil-in-water (O/W) emulsions prepared using starch propionates (DS of 0.64 to 0.86) showed exceptional stability when challenged by centrifugation stress test. These stable O/W emulsions had viscosities in the range of 1236.7–3330.0 mPa·s. In conclusion, moderately substituted short-chain (propionylated) starches could be a promising cold swelling starch, thickener and O/W emulsion stabiliser in food, pharmaceutical and cosmetic industries.U radu su ispitana fizikalno-kemijska svojstva hidroksipropiliranog škroba različitog stupnja supstitucije, te je istražena mogućnost njegove primjene kao stabilizatora emulzija. Djelomično supstituirani škrob pripremljen je esterifikacijom prirodnog škroba s propilen-oksidom, pri čemu je, ovisno o trajanju reakcije, dobiveno dvanaest uzoraka modificiranog škroba stupnja supstitucije od 0,47 do 0,94. Pomoću spektroskopskih metoda FTIR i NMR potvrđena je prisutnost propionskih skupina u strukturi škroba. Rendgenski je difrakcijski uzorak pokazao smanjenje kristaličnosti škroba. Utvrđeno je da se povećanjem stupnja supstitucije škroba proporcionalno povećao i kontaktni kut. Ispitivanjem bubrenja utvrđeno je da modificirani škrob pri niskoj temperaturi (40 °C) jače bubri od prirodnog škroba. Emulzije modificiranog škroba stupnja supstitucije od 0,64 do 0,86 bile su izuzetno stabilne i nakon centrifugiranja, a njihova viskoznost bila je od 1236,7 do 3330,0 MPa•s. Iz rezultata se može zaključiti da se djelomično supstituirani kratkolančani škrob može upotrijebiti kao sredstvo za zgušnjavanje i stabilizator emulzija pri niskim temperaturama u prehrambenoj, farmaceutskoj i kozmetičkoj industriji

Development of a Stepping Force Analgesic Meter for a Rat Arthritic Model

Behavioural assessment of experimental pain is an essential method for analysing and measuring pain levels. Rodent models, which are widely used in behavioural tests, are often subject to external forces and stressful manipulations that cause variability of the parameters measured during the experiment. Therefore, these parameters may be inappropriate as indicators of pain. In this article, a stepping-force analgesimeter was designed to investigate the variations in the stepping force of rats in response to pain induction. The proposed apparatus incorporates new features, namely an infrared charge-coupled device (CCD) camera and a data acquisition system. The camera was able to capture the locomotion of the rats and synchronise the stepping force concurrently so that each step could be identified. Inter-day and intra-day precision and accuracy of each channel (there were a total of eight channels in the analgesimeter and each channel was connected to one load cell and one amplifier) were studied using different standard load weights. The validation studies for each channel also showed convincing results whereby intra-day and inter-day precision were less than 1% and accuracy was 99.36–100.36%. Consequently, an in vivo test was carried out using 16 rats (eight females and eight males). The rats were allowed to randomly walk across the sensor tunnel (the area that contained eight channels) and the stepping force and locomotion were recorded. A non-expert, but from a related research domain, was asked to differentiate the peaks of the front and hind paw, respectively. The results showed that of the total movement generated by the rats, 50.27 ± 3.90% in the case of the male rats and 62.20 ± 6.12% in that of the female rats had more than two peaks, a finding which does not substantiate the assumptions made in previous studies. This study also showed that there was a need to use the video display frame to distinguish between the front and hind paws in the case of 48.80 ± 4.01% of the male rats and 66.76 ± 5.35% of the female rats. Evidently the assumption held by current researchers regarding stepping force measurement is not realistic in terms of application, and as this study has shown, the use of a video display frame is essential for the identification of the front and hind paws through the peak signals

Enteric coating of granules containing the probiotic Lactobacillus acidophilus

In the present study, a capsule formulation composed of enteric coated granules of Lactobacillus acidophilus ATCC 4962 was developed using Eudragit L30D-55 as enteric polymer. Optimization of the capsule formulation was achieved with a maximum viable cell count after 2 h of incubation in acid medium and disintegration time of 1 h in buffer pH 6.8. The amount of Eudragit L30D-55 in the capsules correlated with gastric juice resistance. The best protective qualities against artificial gastric juice were observed when capsules were prepared from granules composed of L. acidophilus, corn starch, lactose monohydrate, polyvinylpyrrolidone and coated with 12.5 % (m/V) of Eudragit L30D-55. Capsule formulation of L. acidophilus in edible broth medium suspension serves as a cheap alternative to the expensive freeze-drying procedure for preparing L. acidophilus. In addition, the enteric coating using Eudragit L30D-55 could protect probiotics from the acidic gastric environment and enhance the bioactivity of probiotics along with replacement of pathogenic microbes in human intestin