Solubility of Drugs in Aqueous Polymeric Solution: Effect of Ovalbumin on Microencapsulation Process

Aziz, Hesham Abdul; Tan, Yvonne Tze Fung; Peh, Kok Khiang

doi:10.1208/s12249-011-9707-x

Cited by 14 publications

(6 citation statements)

References 30 publications

(38 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Owing to increased surface area of the produced nanocrystals, a significant difference (P<0.001) was observed in solubility of the processed ARM compared to the solubility in water and stabilizer solution. There has been previously reported that water soluble polymers and surfactants (HPMC, PVP and SLS) can increase solubility of drug compounds (Aziz, et al, 2012;Leuner and Dressman, 2000). We also observed an increase in solubility of ARM in stabilizer solution (PVA).…”

Section: Solubility Studiessupporting

confidence: 73%

Fabrication and Evaluation of Smart Nanocrystals of Artemisinin for Antimalarial and Antibacterial Efficacy

Shah¹,

Ullah²,

Khan³

et al. 2016

AJTCAM

View full text Add to dashboard Cite

Background: Nanocrystals have the potential to substantially increase dissolution rate, solubility with subsequent enhanced bioavailability via the oral route of a range of poor water soluble drugs. Regardless of other issues, scale up of the batch size is the main issue associated with bottom up approach. Material and Methods: Smart nanocrystals of artemisinin (ARM) was produced relatively at large batch sizes (100, 200, 300 and 400ml) compared to our previously reported study by (Shah, et al., 2016). ARM nanosuspensions/nanocrystals were characterised using zeta sizer, SEM, TEM, DSC, PXRD and RP-HPLC. The nanosuspensions were finally subjected to in vitro antimalarial and antimicrobial activity. Results: The average particle size (PS) for 400 ml batches was 126.5 ±1.02 nm, and the polydispersity index (PI) was 0.194 ± 0.04. The saturation solubility of the ARM nanocrystals was substantially increased to (725.4± 2.0 µg/ml) compared to the raw ARM in water 177.4± 1.3 µg/ml and stabilizer solution (385.3± 2.0 µg/ml). The IC50 value of ARM nanosuspension against P. vivax was 65 and 21 folds lower than micronized 19.5 ng/mL and unprocessed drug (6.4 ng/mL) respectively. The ARM nanosuspension was found highly effective compared to unprocessed drug against all the tested microorganism except E. coli, Shigella and C. albican. Conclusion:The simple precipitation-ultrasonication approach was efficiently employed for fabrication of ARM nanosuspension to scale up the batch size. Similarly, the solubility, antimalarial potential and antimicrobial efficacy of ARM in the form of nanosuspension were significantly enhanced. Findings from this study can persuade research interest for further comprehensive studies using animals model.

show abstract

Section: Solubility Studiessupporting

confidence: 73%

Fabrication and Evaluation of Smart Nanocrystals of Artemisinin for Antimalarial and Antibacterial Efficacy

Shah¹,

Ullah²,

Khan³

et al. 2016

AJTCAM

View full text Add to dashboard Cite

show abstract

“…Despite water-soluble polymers and surfactants such as HPMC, PVP, and SLS being well known to increase the solubility of drug compounds,67,68 the comparison of the solubility profile of the nanosuspension with that of the unprocessed ARTM dissolved in these same surfactants clearly demonstrates that the nanocrystals provide a substantially increased saturation solubility of ARTM. This phenomenon we believe is ascribed to the marked reduction in particle size (=1,000 nm) and the greatly increased surface area of the particles.…”

Section: Resultsmentioning

confidence: 99%

Smart nanocrystals of artemether: fabrication, characterization, and comparative in vitro and in vivo antimalarial evaluation

Shah¹,

Ullah²,

Khan³

et al. 2016

DDDT

View full text Add to dashboard Cite

Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena® DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145.0±2.3 µg/mL) and stabilizer solution (300.0±2.0 µg/mL). The physical stability studies conducted for 90 days demonstrated that nanocrystals stored at 2°C–8°C and 25°C were very stable compared to the samples stored at 40°C. The nanocrystals were also shown to be stable when processed at acidic pH (2.0). The solubility and dissolution rate of ARTM nanocrystals were significantly increased (P<0.05) compared to those of its bulk powder form. The results of in vitro studies showed significant antimalarial effect (P<0.05) against Plasmodium falciparum and Plasmodium vivax. The IC50 (median lethal oral dose) value of ARTM nanocrystals was 28- and 54-fold lower than the IC50 value of unprocessed drug and 13- and 21-fold lower than the IC50 value of the marketed tablets, respectively. In addition, ARTM nanocrystals at the same dose (2 mg/kg) showed significantly (P<0.05) higher reduction in percent parasitemia (89%) against P. vivax compared to the unprocessed (27%), marketed tablets (45%), and microsuspension (60%). The acute toxicity study demonstrated that the LD50 value of ARTM nanocrystals is between 1,500 mg/kg and 2,000 mg/kg when given orally. This study demonstrated that the wet milling technology (Dena® DM-100) can produce smart nanocrystals of ARTM with enhanced antimalarial activities.

show abstract

“…For oral drug delivery, improvement of drug solubility is the main challenge in drug formulations process (Khadka et al, 2014 ). Many approaches had been investigated and applied either alone or in combination for improving the solubility characteristics of poorly water soluble drugs including solvent change co-precipitation (Sertsou et al, 2002 , Khanfar & Salem, 2010 ), solid dispersion (Hosny et al, 2013 ; Maruthapillai et al, 2015 ; Pereira et al, 2016 ), inclusion complexes with β-cyclodextrins (Gao et al, 2012 ; Sambasevam et al, 2013 ; Nair et al, 2014 ), nanosuspensions (Huang et al, 2013 ; Sahu & Das, 2014 ; Gora et al, 2016 ), microencapsulation (Aziz et al, 2012 ), soluble salts formation (Serajuddin, 2007 ), lyophilization (Dixit et al, 2011 ; Dixit & Kulkarni, 2012 ; Xu et al, 2016 ), solubilization (Rangel-Yagui et al, 2005 ; Seedher & Kanojia, 2008 ; Xu et al, 2012 ), and liquisolid technique (Khames, 2013 ; Kamble et al, 2014 ; Sanka et al, 2014 ; Badawy et al, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique

Khames

2017

Drug Delivery

View full text Add to dashboard Cite

To cite this article: Ahmed Khames (2017) Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique, Drug Delivery, 24:1, 328-338, DOI: 10.1080/10717544.2016 Department of Pharmaceutics and Pharmacy Technology, Taif University, Taif, Saudi Arabia Abstract BCS class II drugs usually suffer inadequate bioavailability as dissolution step is the absorption rate limiting step. In this work, the effect of solubility increase at the main absorption site for these drugs was investigated using risperidone as a drug model. Liquisolid technique was applied to prepare risperidone per-oral tablets of high dissolution rate at intestinal pH (6.8) using versatile nonionic surfactants of high solubilizing ability [Transcutol HP, Labrasol and Labrasol/Labrafil (1:1) mixture] as liquid vehicles at different drug concentrations (10-30%) and fixed (R). The prepared liquisolid tablets were fully evaluated and the dissolution rate at pH 6.8 was investigated. The formulae that showed significantly different release rate were selected and subjected to mathematical modeling using DE 25 , MDT and similarity factor (f2). Depending on mathematical modeling results, formula of higher dissolution rate was subjected to solid state characterization using differential scanning calorimetric (DSC), infrared spectroscopy (IR) and X-ray diffraction (XRD). Finally, the drug bioavailability was studied in comparison to conventional tablets in rabbits. Results showed that liquisolid tablet prepared using Labrasol/ Labrafil (1:1) mixture as liquid vehicle containing 10% risperidone is a compatible formula with law drug crystallinity and higher dissolution rate (100% in 25 min). The drug bioavailability was significantly increased in comparison to the conventional tablets (1441.711 mg h/mL and 137.518 mg/mL in comparison to 321.011 mg h/mL and 38.673 mg/mL for AUC and Cp max , respectively). This led to the conclusion that liquisolid technique was efficiently improved drug solubility and solubility increase of BCS class II drugs at their main absorption site significantly increases their bioavailability.

show abstract

Solubility of Drugs in Aqueous Polymeric Solution: Effect of Ovalbumin on Microencapsulation Process

Cited by 14 publications

References 30 publications

Fabrication and Evaluation of Smart Nanocrystals of Artemisinin for Antimalarial and Antibacterial Efficacy

Fabrication and Evaluation of Smart Nanocrystals of Artemisinin for Antimalarial and Antibacterial Efficacy

Smart nanocrystals of artemether: fabrication, characterization, and comparative in vitro and in vivo antimalarial evaluation

Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique

Contact Info

Product

Resources

About