scholarly journals Biocatalytic Approach for Direct Esterification of Ibuprofen with Sorbitol in Biphasic Media

2021 ◽  
Vol 22 (6) ◽  
pp. 3066
Author(s):  
Federico Zappaterra ◽  
Maria Elena Maldonado Rodriguez ◽  
Daniela Summa ◽  
Bruno Semeraro ◽  
Stefania Costa ◽  
...  
Keyword(s):  
Drug Product ◽  
Critical Role ◽  
Water Soluble ◽  
Esterification Reaction ◽  
Enzymatic Esterification ◽  
Porcine Pancreas ◽  
Direct Esterification ◽  
Water Soluble Drug ◽  
Anti Inflammatory ◽  
The 1960S

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) introduced in the 1960s and widely used as an analgesic, anti-inflammatory, and antipyretic. In its acid form, the solubility of 21 mg/L greatly limits its bioavailability. Since the bioavailability of a drug product plays a critical role in the design of oral administration dosage, this study investigated the enzymatic esterification of ibuprofen as a strategy for hydrophilization. This work proposes an enzymatic strategy for the covalent attack of highly hydrophilic molecules using acidic functions of commercially available bioactive compounds. The poorly water-soluble drug ibuprofen was esterified in a hexane/water biphasic system by direct esterification with sorbitol using the cheap biocatalyst porcine pancreas lipase (PPL), which demonstrated itself to be a suitable enzyme for the effective production of the IBU-sorbitol ester. This work reports the optimization of the esterification reaction.

scholarly journals Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies

Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 791
Author(s):  
Tamer M. Shehata ◽  
Mahmoud M. Ibrahim ◽  
Heba S. Elsewedy
Keyword(s):  
Tween 80 ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Skin Permeability ◽  
Water Soluble Drug ◽  
Anti Inflammatory ◽  
Niosomal Gel ◽  
Span 60

Curcumin is a poorly water-soluble drug that is used for the treatment of inflammations, tumors, wound healing antioxidant and other diseases. In the current manuscript, it is successfully formulated into proniosome gels. The proniosomes are readily hydrated into niosomal formulations using warm water. Proniosomes were prepared using nonionic surfactants (tween 80, span 60) either solely or in combinations with cholesterol. The produced niosomal formulations were homogenous in size with vesicular sizes >343 and <1800 nm. The encapsulation efficiency percentage “EE%” of curcumin in niosomal formulations was different according to niosomal composition. It increased up to 99.74% in formulations of tween 80/Chol of 200 μmole/mL lipid concentration. Span 60/chol niosomes showed decreased curcumin EE%. Niosomal formulations showed increased SSTF and PC with enhancement ratios of more than 20-fold compared with curcumin suspension form. Kinetically, niosomes fitted to the Korsemeyer-Peppas model with non-Fickian transport according to their calculated n-values where curcumin suspension form showed Korsemeyer-Peppas kinetics with Fickian transport. Niosomal formulations deposited higher curcumin amounts in the skin compared with the suspension form. The best niosomal formulation (F9) was used for niosomal gel and emulgel fabrication. Finally, the anti-inflammatory activity of curcumin in various formulations was evaluated using a rat hind paw edema method and the % of swelling was 17.5% following 24 h in group treated with curcumin niosomal emulgel. In conclusion, this study suggests that the developed niosomal emulgel could significantly enhance the anti-inflammatory effect of curcumin and be an efficient carrier for the transdermal delivery of the drug.

scholarly journals Enlarged Pore Size Chiral Mesoporous Silica Nanoparticles Loaded Poorly Water-Soluble Drug Perform Superior Delivery Effect

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3552 ◽  
Author(s):  
Yingyu Guo ◽  
Kaijun Gou ◽  
Baixue Yang ◽  
Yumei Wang ◽  
Xueyu Pu ◽  
...  
Keyword(s):  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Delivery System ◽  
Mesoporous Silica Nanoparticles ◽  
Water Soluble ◽  
Synthesis Process ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Anti Inflammatory ◽  
Poorly Water Soluble Drug

Large mesopores of chiral silica nanoparticles applied as drug carrier are worth studying. In this study, chiral mesoporous silica nanoparticles (CMSN) and enlarged chiral mesoporous silica nanoparticles (E-CMSN) with a particle size from 200 to 300 nm were synthesized. Fourier transform infrared spectrometer (FTIR), circular dichroism spectrum, scanning electron microscopy (SEM), transmission electron microscope (TEM), and nitrogen adsorption/desorption measurement were adopted to explore their characteristics. The results showed that the surface area, pore volume, and pore diameter of E-CMSN were higher than those of CMSN due to enlarged mesopores. Poorly water-soluble drug nimesulide (NMS) was taken as the model drug and loaded into carriers using adsorption method. After NMS was loaded into CMSN and E-CMSN, most crystalline NMS converted to amorphous phase and E-CMSN was superior. The anti-inflammatory pharmacodynamics and in vivo pharmacokinetics results were consistent with the wetting property and in vitro drug dissolution results, verifying that NMS/E-CMSN exhibited superior NMS delivery system based on its higher oral relative bioavailability and anti-inflammatory effect because its enlarge mesopores contributed to load and release more amorphous NMS. The minor variations in the synthesis process contributed to optimize the chiral nano-silica drug delivery system.

scholarly journals Water-soluble C60 fullerene ameliorates astroglial reactivity and TNFa production in retina of diabetic rats

2019 ◽  
Vol 10 (4) ◽  
pp. 513-519 ◽  
Author(s):  
V. S. Nedzvetsky ◽  
E. V. Sukharenko ◽  
G. Baydas ◽  
G. V. Andrievsky
Keyword(s):  
Critical Role ◽  
Diabetic Rats ◽  
Fullerene C60 ◽  
Water Soluble ◽  
C60 Fullerene ◽  
Diabetic Rat ◽  
Retinal Cells ◽  
Diabetes Model ◽  
Anti Inflammatory ◽  
Glial Reactivity

The complications of both first and second types of diabetes mellitus patients are important cause of decline in quality of life and mortality worldwide. Diabetic retinopathy (DR) is a widespread complication that affects almost 60% of patients with prolonged (at least 10–15 years) diabetes. The critical role of glial cells has been shown in retinopathy initiation in the last decades. Furthermore, glial reactivity and inflammation could be key players in early pathogenesis of DR. Despite the large amount of research data, the approaches of effective DR therapy remain unclear. The progress of DR is accompanied by pro-inflammatory and pro-oxidative changes in retinal cells including astrocytes and Muller cells. Glial reactivity is a key pathogenetic factor of various disorders in neural tissue. Fullerene C60 nanoparticles were confirmed for both antioxidant and anti-inflammatory capability. In the presented study glioprotective efficacy of water-soluble hydrated fullerene C60 (C60HyFn) was tested in a STZ-diabetes model during 12 weeks. Exposure of the STZ-diabetic rat group to C60HyFn ameliorated the astrocyte reactivity which was determined via S100β and PARP1 overexpression. Moreover, C60HyFn induced the decrease of TNFα production in the retina of STZ-diabetic rats. By contrast, the treatment with C60HyFn of the normal control rat group didn’t change the content of all abovementioned markers of astrogliosis and inflammation. Thus, diabetes-induced abnormalities in the retina were suppressed via the anti-oxidant, anti-inflammatory and glioprotective effects of C60HyFn at low doses. The presented results demonstrate that C60HyFn can ensure viability of retinal cells viability through glioprotective effect and could be a new therapeutic nano-strategy of DR treatment.

scholarly journals Glyceric Prodrug of Ursodeoxycholic Acid (UDCA): Novozym 435-Catalyzed Synthesis of UDCA-Monoglyceride

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5966
Author(s):  
Federico Zappaterra ◽  
Stefania Costa ◽  
Daniela Summa ◽  
Bruno Semeraro ◽  
Virginia Cristofori ◽  
...  
Keyword(s):  
Bile Acid ◽  
Ursodeoxycholic Acid ◽  
Bile Acids ◽  
Immobilized Lipase ◽  
Critical Role ◽  
Clinical Effectiveness ◽  
Water Soluble ◽  
Novozym 435 ◽  
Biliary Cirrhosis ◽  
Enzymatic Esterification

Bile acids (BAs) are a family of steroids synthesized from cholesterol in the liver. Among bile acids, ursodeoxycholic acid (UDCA) is the drug of choice for treating primary biliary cirrhosis and dissolving cholesterol gallstones. The clinical effectiveness of UDCA includes its choleretic activity, the capability to inhibit hydrophobic bile acid absorption by the intestine under cholestatic conditions, reducing cholangiocyte injury, stimulation of impaired biliary output, and inhibition of hepatocyte apoptosis. Despite its clinical effectiveness, UDCA is poorly soluble in the gastro-duodeno-jejunal contents, and pharmacological doses of UDCA are not readily soluble in the stomach and intestine, resulting in incomplete absorption. Indeed, the solubility of 20 mg/L greatly limits the bioavailability of UDCA. Since the bioavailability of drug products plays a critical role in the design of oral administration dosages, we investigated the enzymatic esterification of UDCA as a strategy of hydrophilization. Therefore, we decided to enzymatically synthesize a glyceric ester of UDCA bile acid to produce a more water-soluble molecule. The esterification reactions between UDCA and glycerol were performed with an immobilized lipase B from Candida antarctica (Novozym 435) in solvent-free and solvent-assisted systems. The characterization of the UDCA-monoglyceride, enzymatically synthesized, has been performed by 1H-NMR, 13C-NMR, COSY, HSQC, HMBC, IR, and MS spectroscopy.

Formulation Development of Aceclofenac Nanosuspension as an Alternative Approach for Improving Drug Delivery of Poorly Soluble Drugs

2013 ◽  
Vol 6 (3) ◽  
pp. 2145-2153
Author(s):  
S. Lakshmana Prabu ◽  
S P Sharavanan ◽  
S Govindaraju ◽  
T N K Suriyaprakash
Keyword(s):  
Dissolution Rate ◽  
Drug Formulation ◽  
Water Soluble ◽  
Therapeutic Drug ◽  
Formulation Development ◽  
Water Soluble Drug ◽  
Study Results ◽  
Poorly Water Soluble ◽  
Anti Inflammatory ◽  
Poorly Water Soluble Drug

Poor water solubility of active pharmaceutical ingredients is a major problem in drug discovery and formulation development. Nanoparticle engineering process has been seen as a promising approach for the enhancement of drug solubility. In this study, we present an approach of nanosizing a drug/polymeric complex to increase both solubility and dissolution rate of poorly-water soluble drug aceclofenac, which is widely used as anti-inflammatory drug. Polymeric nanosuspensions were prepared by nanoprecipitation method by using biodegradable polymer loaded with aceclofenac, with the aim to improve anti-inflammatory therapy. The prepared formulation was evaluated for drug excipients compatibility study, polydispersity index, particle size analysis, surface morphology, zeta potential, drug release features and stability. These study results indicate the suitability of formulation procedure for preparation of nanosized poorly-water soluble drug formulation with significantly improved in vitro dissolution rate and fast onset of therapeutic drug effect.

The fixation of a water-soluble drug in calcium-induced alginate gel beads and the release profiles from the vehicle.

1997 ◽  
Vol 12 (1) ◽  
pp. 49-55 ◽  
Author(s):  
Yoshifumi Murata ◽  
Norie Katayana ◽  
Takashi Kajita ◽  
Etsuko Miyamoto ◽  
Susumu Kawashima
Keyword(s):  
Water Soluble ◽  
Alginate Gel ◽  
Gel Beads ◽  
Water Soluble Drug ◽  
Release Profiles

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

2015 ◽  
Vol 8 (4) ◽  
pp. 3053-3059
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
H G Sandip
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Water Soluble ◽  
Wet Granulation ◽  
Wetting Properties ◽  
Enhanced Dissolution ◽  
Water Soluble Drug ◽  
Drug Concentrations ◽  
Water Soluble Drugs ◽  
Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.  

Sign in / Sign up

Export Citation Format

Share Document