Hydroxypropyl Β-cyclodextrin Research Articles

Design Strategy for Vulcanization Accelerator of Diphenylguanidine/Cyclodextrin Inclusion Complex for Natural Rubber Latex Foam with Enhancing Performance.

Vulcanization is an essential process to obtain high-performance rubber products. Diphenylguanidine (DPG) is often used as the secondary accelerator in the vulcanization process of natural rubber (NR) latex. However, DPG would make NR latex emulsion exhibit gelation, resulting in the negative vulcanization efficiency. In addition, exposure to DPG might lead to some physiological diseases during the production process of DPG doped NR latex. Hydroxypropyl-β-cyclodextrin (HP-β-CD) with the hydrophobic interior and hydrophilic exterior has the advantages of good water solubility, high bioavailability, reliable stability, and low toxicity. In this study, the inclusion complex of diphenylguanidine-hydroxypropyl-β-cyclodextrin (DPG-HP-β-CD) is prepared by ball milling with a host-guest molar ratio of 1 : 1, which has also been applied to the foaming process of NR latex. The mechanical properties of DPG-HP-β-CD inclusion complex/natural rubber latex foam (DPG-HP-β-CD/NRLF) have been significantly improved, including the tensile strength, elongation at break, hardness, compression set, resilience, and antiaging performance. Further, the usage of DPG has been reduced, leading to the reduction of toxicity and environmental hazards.

Mitigating RANKL-induced cholesterol overload in macrophages with β-cyclodextrin-threaded polyrotaxanes suppresses osteoclastogenesis.

Free cholesterol acts as an endogenous agonist for estrogen-related receptor α (ERRα), a nuclear receptor that regulates osteoclastogenesis. Because stimulation of macrophages with receptor activator of nuclear factor κB ligand (RANKL) induces an overload of free cholesterol and activates ERRα, we hypothesized that direct removal of cellular cholesterol would suppress osteoclastogenesis. In this study, the effect of 2-hydroxypropyl β-cyclodextrin (HP-β-CD), a highly water-soluble cyclic glucopyranose, and β-CD-threaded polyrotaxanes (PRXs), supramolecular polymers designed to release threaded β-CDs in acidic lysosomes, on RANKL-induced cholesterol overload and osteoclast differentiation of murine macrophage-like RAW264.7 cells were investigated. PRXs suppressed RANKL-induced cholesterol overload. Additionally, RANKL-induced osteoclast differentiation of RAW264.7 cells was inhibited by PRXs. In contrast, HP-β-CD did not reduce cholesterol levels or inhibit osteoclast differentiation in RAW264.7 cells. Gene expression analysis of osteoclast markers suggested that PRXs suppress only the early stage of osteoclast differentiation, as PRXs cannot be internalized into multinucleated osteoclasts. However, modification of PRXs with cell-penetrating peptides facilitated their cellular uptake into multinucleated osteoclasts and inhibited osteoclast maturation. Thus, PRXs are promising candidates for inhibiting osteoclast differentiation by suppressing cholesterol overload and may be useful for treating osteoporosis or other bone defects caused by the overactivity of osteoclasts.

Oral Treatment with Angiotensin-(1-7) Attenuates the Kidney Injury Induced by Gentamicin in Wistar Rats.

Acute Kidney Injury (AKI), a common disease of the urinary system, can be induced by high doses of gentamicin (GM). The renin-angiotensin system exerts a key role in the progression of the AKI since elevated intrarenal levels of Ang II, and ACE activity is found in this condition. However, it is unknown whether oral administration of angiotensin (Ang)-(1-7), a heptapeptide that evokes opposite effects of Ang II, may attenuate the renal injuries induced by gentamicin. To evaluate the effects of Ang-(1-7) on GM-induced renal dysfunction in rats. AKI was induced by subcutaneous administration of GM (80 mg/Kg) for 5 days. Simultaneously, Ang-(1-7) included in hydroxypropyl β-cyclodextrin (HPβCD) was administered by gavage [46 μg/kg HPβCD + 30 μg/kg Ang-(1-7)]. At the end of the treatment period (sixth day), the rats were housed in metabolic cages for renal function evaluation. Thereafter, blood and kidney samples were collected. Ang-(1-7) attenuated the increase of the plasmatic creatinine and proteinuria caused by GM but did not change the glomerular filtration rate nor tubular necrosis. Ang-(1-7) attenuated the increased urinary flow and the fractional excretion of H2O and potassium observed in GM rats but intensified the elevated excretion of sodium in these animals. Morphological analysis showed that Ang-(1-7) also reduced the tubular vacuolization in kidneys from GM rats. Ang-(1-7) promotes selective beneficial effects in renal injuries induced by GM.

A simple and cost-effective synthesis of sulfated β-cyclodextrin and its application as chiral mobile phase additive in the separation of cloperastine enantiomers

A simple and cost-effective method for the synthesis of sulfated β-cyclodextrin, one of the most widely used chiral mobile phase additives, using sulfamic acid as a sulfonating agent has been described. The method was optimized, and the synthesized product was characterized by spectroscopic, size-exclusion chromatographic, thermal, and microscopic methods and was compared to the marketed Sigma Aldrich sulfated β-cyclodextrin. β-Cyclodextrin, hydroxypropyl β-cyclodextrin, sulfated β-cyclodextrin (marketed and synthesized) were evaluated as chiral mobile phase additives for the enantiomeric separation of cloperastine, an antitussive agent, using reversed-phase HPLC. Under optimized conditions, a resolution of 3.14 was achieved within 15 min on an achiral Kromasil C8 (150 × 4.6 mm, 5 µm) column, with 5 mM monopotassium phosphate containing 10 mM synthesized sulfated β-cyclodextrin pH 3.0 and 45% methanol as mobile phase. The method utilizing synthesized sulfated β-cyclodextrin as chiral mobile phase additive was validated as per ICH guidelines and applied for the quantitative determination of cloperastine enantiomers in active pharmaceutical ingredients and pharmaceutical formulations. The selectivity changes imparted by sulfated β-cyclodextrin were proven to be beneficial for chiral separation. For the enantiomeric separation of cloperastine, synthesized sulfated β-cyclodextrin afforded better resolution than marketed sulfated β-cyclodextrin.

Effect of Molar Mass of Hydroxypropyl β-cyclodextrin on the Aqueous Solubility of Dimenhydrinate

Effect of Molar Mass of Hydroxypropyl β-cyclodextrin on the Aqueous Solubility of Dimenhydrinate

Comparing the extraction performance of cyclodextrin-containing supramolecular deep eutectic solvents versus conventional deep eutectic solvents by headspace single drop microextraction

A headspace single drop microextraction (HS-SDME) method coupled with high performance liquid chromatography was developed to compare the extraction of eighteen aromatic organic pollutants from aqueous solutions using cyclodextrin-based supramolecular deep eutectic solvents (SUPRADESs) and alkylammonium halide-based conventional deep eutectic solvents (DESs). Different derivatives of beta-cyclodextrin (β-CD) were employed as hydrogen bond acceptors (HBA) in SUPRADESs and the extraction performance investigated. SUPRADES comprised of the 20 wt% native β-CD HBA provided the highest enrichment factors of analytes compared to SUPRADESs comprised of other derivatives of β-CD (random methylated β-cyclodextrin, heptakis(2,3,6-tri-O-methyl)-β-cyclodextrin, and 2-hydroxypropyl β-cyclodextrin). In addition, native β-CD and its derivatives were dissolved in the neat DESs and their effect on the extraction of analytes examined. Dissolution of 20 wt% native β-CD in the choline chloride ([Ch+][Cl−]):2Urea DES resulted in a significant increase in the extraction efficiencies of target analytes compared to the neat [Ch+][Cl−]:2Urea DES. Under optimum conditions, the extraction method required a solvent microdroplet of 6.5 μL, 1000 rpm stir rate, 30% (w/v) salt concentration, and a temperature of 40 °C. The tetrabutylammonium chloride: 2 lactic acid DES resulted in the highest enrichment factors while the [Ch+][Cl−]:2Urea DES had the lowest for most of the analytes among the evaluated solvents. The method provided limits of detection (LODs) down to 35 μg L−1. Furthermore, the developed method was applied for the analysis of spiked tap and lake water, where relative recoveries ranging from 83.7% ̶ 119.7% and relative standard deviations lower than 19.2% were achieved.

Magnetic poly(β-cyclodextrin) combined with solubilizing agents for the rapid bioaccessibility measurement of polycyclic aromatic hydrocarbons in soils

The rapid determination of the bioaccessibility of polycyclic aromatic hydrocarbons (PAHs) in soils is challenging due to their slow desorption rates and the insufficient extraction efficiency of the available methods. Herein, magnetic poly(β-cyclodextrin) microparticles (Fe3O4@PCD) were combined with hydroxypropyl-β-cyclodextrin (HPCD) or methanol (MeOH) as solubilizing agents to develop a rapid and effective method for the bioaccessibility measurement of PAHs. Fe3O4@PCD was first validated for the rapid and quantitative adsorption of PAHs from MeOH and HPCD solutions. The solubilizing agents were then coupled with Fe3O4@PCD to extract PAHs from soil-water slurries, affording higher extractable fractions than the corresponding solution extraction and comparable to or higher than single Fe3O4@PCD or Tenax extraction. The desorption rates of labile PAHs could be markedly accelerated in this process, which were 1.3–12.0 times faster than those of single Fe3O4@PCD extraction. Moreover, a low HPCD concentration was sufficient to achieve a strong acceleration of the desorption rate without excessive extraction of the slow desorption fraction. Finally, a comparison with a bioaccumulation assay revealed that the combination of Fe3O4@PCD with HPCD could accurately predict the PAH concentration accumulated in earthworms in three field soil samples, indicating that the method is a time-saving and efficient procedure to measure the bioaccessibility of PAHs.

Characterization of chitosan film with cinnamon essential oil emulsion co-stabilized by ethyl-Nα-lauroyl-l-arginate hydrochloride and hydroxypropyl-β-cyclodextrin

To improve the antimicrobial properties of chitosan films, cinnamon essential oil (CEO) nanoemulsion (1% and 3% v/v CEO) stabilized by ethyl-Nα-lauroyl-l-arginate hydrochloride (LAE) alone or co-stabilized by LAE and hydroxypropyl-β-cyclodextrin (HPCD) were incorporated into chitosan matrix. The micromorphology, physical and antimicrobial properties of the composite films were compared. The dense structure of the CEO nanoemulsion co-stabilized by LAE and HPCD reduced the water vapor permeability and water content. The incorporation of the CEO nanoemulsion co-stabilized by LAE and HPCD, reduced the adverse effects of CEO on the mechanical properties and microstructure of the film, and even slightly increased the tensile strength. In addition, the antimicrobial properties of chitosan films were enhanced due to the encapsulation and emulsification effect of HPCD and LAE on CEO. This work indicated that the prepared chitosan based edible films had the potential to be used in the field of food packaging to improve food safety.

Nanoemulsion of cinnamon essential oil Co-emulsified with hydroxypropyl-β-cyclodextrin and Tween-80: Antibacterial activity, stability and slow release performance

Essential oils (EOs) are gaining great interest as alternatives to synthetic food preservatives due to their antimicrobial activity. However, EOs are hydrophobic and easy to evaporate. In this research, EOs were encapsulated in nanoemulsions with the aid of hydroxypropyl-β-cyclodextrin (HPCD) to protect the ingredients and sustain the release, so as to exert long-term antibacterial effects. The influence of HPCD and its concentration on cinnamon essential oil (CEO) nanoemulsion formation, antibacterial activity, release property and stability was investigated. The results showed that HPCD reduced the particle size of nanoemulsion as the concentration of Tween 80 ranged from 2 to 4 g/L. However, HPCD addition showed adverse effect as the content of Tween 80 was 5 g/L. Antibacterial tests against Escherichia coli and Staphylococcus aureus demonstrated that the addition of HPCD contributed to the increase of antimicrobial activity of CEO nanoemulsions and showed the best effect when the concentration of HPCD was 30 g/L. The release experiment proved the slow-release ability of HPCD, and showed that the cavity of HPCD helped to reduce the loss of CEO, thus delayed the release time and enhanced the antibacterial effect. Meanwhile, the use of HPCD contributed to the storage stability of the emulsion at 4, 25, and 40 °C, and the nanoemulsion remained stable during a storage period of 60 days.

Monodispersed cyclodextrin-based nanocomplex of neuropeptide Y for targeting MCF-7 cells using a central composite design

The present study aimed to complex neuropeptide Y with hydroxypropyl β-cyclodextrin (HPβ-CD) and optimize using central composite design with different levels of neuropeptide Y and HPβ-CD. The validated inclusion nanocomplex (formulation CN) showed monodispersed particle size of 330.019 ± 4.08 nm, % entrapment efficiency of 84.68 ± 5.47 and in-vitro neuropeptide Y release from the complex of 85.16 ± 6.13% for 24 h. Formulation CN was found to be stable for 3 months under two conditions: 1) 5 ± 2 °C with relative humidity 80 ± 5% and 2) 25 ± 2 °C with relative humidity 60 ± 5%. It showed apoptosis of 67.38 ± 7.54% and IC50 value of 0.8 ± 0.005 μg/mL on MCF-7 cell lines via MAPK pathway and interference with cell membrane for reduction in the cell proliferation. The cell cycle analysis inferred G0G1 phase arrest (23.63 ± 5.12%) by formulation CN due to intervention of neuropeptide Y for inhibition of cell growth. Hence, the results displayed that neuropeptide Y nanocomplex is considered as a promising peptide delivery in breast cancer treatment in a controlled manner.

Oral administration of angiotensin-(1-7) decreases muscle damage and prevents the fibrosis in rats after eccentric exercise.

What is the central question of this study? Eccentric contraction exercises cause damage to muscle fibres and induce inflammatory responses. The exacerbation of this process can induce deposition of fibrous connective tissue, leading to decreased muscle function. The aim of this study was to examine the role of angiotensin-(1-7) in this context. What is the main finding and its importance? Our results show that oral treatment with angiotensin-(1-7) decreases muscle damage induced by eccentric exercise, reducing inflammation and fibrosis in the gastrocnemius and soleus muscles. This study shows a potential effect of angiotensin-(1-7) for the prevention of muscle injuries induced by physical exercise. Eccentric contraction exercises cause damage to the muscle fibres and induce an inflammatory reaction. The protective effect of angiotensin-(1-7) [Ang-(1-7)] in skeletal muscle has led us to examine the role of this peptide in modifying processes associated with inflammation and fibrogenesis induced by eccentric exercise. In this study, we sought to investigate the effects of oral administration of Ang-(1-7) formulated in hydroxypropyl β-cyclodextrin (HPβ-CD) in prevention and treatment of muscle damage after downhill running. Male Wistar rats were divided into three groups: control (untreated and not exercised; n=10); treated/exercised HPβ-CD Ang-(1-7) (n=40); and treated/exercised HPβ-CD (n=40). Exercised groups were subjected to a single eccentric contraction exercise session on a treadmill inclined to -13° at a constant speed of 20m/min, for 60min. Oral administration of HPβ-CD Ang-(1-7) and HPβ-CD was performed 3 h before the exercise protocol and daily as a single dose, until the end of the experiment. Samples were collected 4, 12, 24, 48 and 72h after the exercise session. The animals treated with the Ang-(1-7) showed lower levels of creatine kinase, lower levels of tumor necrosis factor-α in soleus muscle and increased levels of interleukin-10 cytokines. The inflammatory cells and deposition of fibrous connective tissue in soleus and gastrocnemius muscles were lower in the group treated with Ang-(1-7). The results of this study show that treatment with an oral formulation of Ang-(1-7) enhances the process of repair of muscle injury induced by eccentric exercise.

Targeting hypoxia for sensitization of tumors to apoptosis enhancement through supramolecular biohybrid bacteria

Bacteria-driven drug-delivery systems have drawn considerable interests for their highly selective hypoxia-targeting and efficacy in tumor inhibition. For the first time, a supramolecular biohybrid bacterium (SA@HU) is constructed by coating attenuated Salmonella typhimurium (S. typhimurium ΔppGpp/Lux) with nanoassemblies. In addition, the host–guest inclusion complexes based on hydroxypropyl-β-cyclodextrin (HPCD) and amantadine (AMA) was developed to encapsulate the natural antineoplastic product, ursolic acid (UA). It is found that the drug-carried coating layer has no significant impact on the antitumor activity or tumor-targeting capacity of bacteria. Significant restraint of tumor progression is achieved by SA@HU due to the synergy of cellular immune activation and apoptosis enhancement. Most importantly, intravenous delivery of UA by this biohybrid vector can cause tumor lysis, as the bacteria-attracting nutrients beneficial for preferential accumulation of bacteria in tumor. The mutual promotion of bacteria and UA may also contribute to a superior anticancer effect. Hence, the SA@HU-based biotic/abiotic supramolecular therapeutic system represents a novel strategy for combined chemo-bacterial therapy.

Changes and release risk of typical pharmaceuticals and personal care products in sewage sludge during hydrothermal carbonization process

Hydrochars were obtained by hydrothermal carbonization treatment of municipal sewage sludge. Effects of reaction temperature (180–300 °C) and reaction time (2–15 h) on structural characteristics of the hydrochars, and changes and release risk of typical pharmaceuticals and personal care products (PPCPs) in the hydrochars were investigated. Reaction temperature played a more important role than reaction time on hydrochar properties and decarboxylation reaction was the primary process during the converting of sludge to hydrochars. The sludge hydrochars had higher yields, carbon recovery rates, polarity and less aromaticity than biochars. Hydrothermal process reduced PPCPs’ load in sludge hydrochars effectively except caffeine and acetaminophen. The hydrochars prepared at intermediate and high temperatures (240 and 300 °C) had higher caffeine concentrations than the original sludge, which can be ascribed to the transformation of N-containing precursors. The highest CaCl2 extracted caffeine concentration occurred at intermediate temperature of 240 °C (48.1 μg/kg) due to the stronger affinity of caffeine in the high-temperature hydrochars. Caffeine was not detected in hydroxypropyl-β-cyclodextrin (HPCD) extract. Hydrochars prepared at low temperature (180 °C) had a higher acetaminophen concentration than the original sludge, which was attributed to the high thermal stability temperature of acetaminophen. Low- and intermediate-temperature hydrochars had higher CaCl2 extracted acetaminophen concentrations. The HPCD extracted acetaminophen was low with a range of nd to 6.72 μg/kg. In conclusion, PPCPs are less likely to constitute a limiting factor on the farm application of sludge hydrochar. This study provides theoretical support for the safe application of sludge hydrochar in the farmland.

Improved quantification of N-methylcarbamates combining supramolecular post-column derivatization-fluorescence detection-high performance liquid chromatography and partial least squares analysis

A strategy to improve the simultaneous quantification of N-methyl-carbamate pesticides was performed. It takes advantage of the supramolecular interactions between the analytes and hydroxypropyl-β-cyclodextrin (HPCD) in the post-column reactor to increase the high-performance liquid chromatography-fluorescence sensitivity and use the partial least squares algorithm for the data analysis to identify strong overlap signals. The use of HPCD in the derivatization reactor generated a 50% of improvement in the limit of detection of Aminocarb (11.29 ng/ mL), Carbofuran (CF) (19.58 ng/mL) and, Bendiocarb (BC) (0.27 mg/mL). It practically was the same for Carbaryl (2.35 ng/mL), but with a precise identification between CF and BC. The methods developed for these analytes were exactly on the elliptic joint confidence region. The recoveries in domiciliary water indicate the accuracy of the methodologies developed with values between 97% and 103% at the maximum concentration levels allow by international recommendations..

Preparation of astaxanthin micelles self-assembled by a mechanochemical method from hydroxypropyl β-cyclodextrin and glyceryl monostearate with enhanced antioxidant activity

This research aimed to overcome the current challenges in the application of natural carotenoid antioxidants, such as their complex preparation processes, low bioavailability and poor drug stability. Herein, a mechanochemical method was used to prepare an inclusion complex (IC) that self-assembles into micelles in aqueous solution and achieves solid-phase loading of astaxanthin (AST). The NMR analysis, thermodynamics study, particle size analysis and electron microscopy image results showed that AST, hydroxypropyl β-cyclodextrin (HPβ-CD) and glyceryl monostearate (GMS) formed self-assembled micelles and maintained good stability in aqueous solution. The antioxidant performance experiments showed that the formation of IC increases free radical scavenging activity. The pharmacokinetic studies showed that the bioavailability of the astaxanthin inclusion complex increased 4-fold. The tissue distribution experiments showed that the astaxanthin inclusion complex targets the liver to exert its antioxidant effects. The proposed method uses an innovative preparation technology to produce an efficient drug delivery system without solvents, and it exerts powerful antioxidant activity against astaxanthin.

Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability.

To improve physicochemical properties of vardenafil hydrochloride (VAR), its amorphous form and combinations with excipients—hydroxypropyl methylcellulose (HPMC) and β-cyclodextrin (β-CD)—were prepared. The impact of the modification on physicochemical properties was estimated by comparing amorphous mixtures of VAR to their crystalline form. The amorphous form of VAR was obtained as a result of the freeze-drying process. Confirmation of the identity of the amorphous dispersion of VAR was obtained through the use of comprehensive analysis techniques—X-ray powder diffraction (PXRD) and differential scanning calorimetry (DSC), supported by FT-IR (Fourier-transform infrared spectroscopy) coupled with density functional theory (DFT) calculations. The amorphous mixtures of VAR increased its apparent solubility compared to the crystalline form. Moreover, a nearly 1.3-fold increase of amorphous VAR permeability through membranes simulating gastrointestinal epithelium as a consequence of the changes of apparent solubility (Papp crystalline VAR = 6.83 × 10−6 cm/s vs. Papp amorphous VAR = 8.75 × 10−6 cm/s) was observed, especially for its combinations with β-CD in the ratio of 1:5—more than 1.5-fold increase (Papp amorphous VAR = 8.75 × 10−6 cm/s vs. Papp amorphous VAR:β-CD 1:5 = 13.43 × 10−6 cm/s). The stability of the amorphous VAR was confirmed for 7 months. The HPMC and β-CD are effective modifiers of its apparent solubility and permeation through membranes simulating gastrointestinal epithelium, suggesting a possibility of a stronger pharmacological effect.

The effect of drug loading on the properties of abiraterone–hydroxypropyl beta cyclodextrin solid dispersions processed by solvent free KinetiSol® technology

Abiraterone is a poorly water-soluble drug used in the treatment of prostate cancer. In our previous study, we reported that KinetiSol® processed solid dispersions (KSDs) based on hydroxypropyl β-cyclodextrin (HPBCD) showed improved dissolution and pharmacokinetics of abiraterone. However, the nature of abiraterone-HPBCD interaction within the KSDs or the effect of drug loading on the physicochemical properties and in vivo performance of HPBCD-based KSDs remain largely unknown. We hypothesize that KinetiSol technology can prepare abiraterone-HPBCD complexes within KSDs and that increasing the drug loading beyond an optimal point reduces the in vitro and in vivo performance of these KSDs. To confirm our hypothesis, we developed KSDs with 10–50% w/w drug loading and analyzed them using X-ray diffractometry and modulated differential scanning calorimetry. We found that KSDs containing 10–30% drug were amorphous. Interestingly, two-dimensional solid-state nuclear magnetic resonance and Raman spectroscopy indicated that the abiraterone-HPBCD complexes were formed. At elevated temperatures, the 10% and 20% drug-loaded KSDs were physically stable, while the 30% drug-loaded KSD showed recrystallization of abiraterone. In vitro dissolution and in vivo pharmacokinetic performances improved as the drug loading decreased; we attribute this to increased noncovalent interactions between abiraterone and HPBCD at lower drug loadings. Overall, the 10% drug loaded KSD showed a dissolution enhancement of 15.7-fold compared to crystalline abiraterone, and bioavailability enhancement of 3.9-fold compared to the commercial abiraterone acetate tablet Zytiga®. This study is first to confirm that KinetiSol, a high-energy, solvent-free technology, is capable of forming abiraterone-HPBCD complexes. Furthermore, in terms of in vitro and in vivo performance, a 10% drug load is optimal.

Bioaugmentation treatment of polycyclic aromatic hydrocarbon-polluted soil in a slurry bioreactor with a bacterial consortium and hydroxypropyl-β-cyclodextrin

ABSTRACT The aim of the study was to verify the effect of bioaugmentation by the bacterial consortium YS with hydroxypropyl-β-cyclodextrin (HPCD) in a soil slurry. The bacterial consortium YS was enriched from a petroleum-polluted soil using pyrene as sole carbon resource. After 3 weeks, the degradation rate of phenanthrene in CK increased from 22.58% to 55.23 and 78.21% in bioaugmentation (B) and HPCD + bioaugmentation (MB) respectively. The degradation rate of pyrene in CK increased from 17.33% to 51.10% and 60.32% in B and MB respectively in the slurry. The augmented YS persisted in the slurry as monitored by 16S rRNA gene high-throughput sequencing and outcompeted some indigenous bacteria. Enhanced polycyclic aromatic hydrocarbon (PAH) degradation was observed in the addition of HPCD due to the enhanced bioavailability of phenanthrene and pyrene. Additionally, the amount of PAH-degrading bacteria and enzymatic activity in bioaugmentation with HPCD were higher than that in the CK group. The results indicated that bioaugmentation with a bacterial consortium and HPCD is an environmentally friendly method for the bioremediation of PAH-polluted soil.

Temporal changes in the extractability, bioaccessibility and biodegradation of target hydrocarbons in soils from former refinery facilities

This study investigated the extractability, bioaccessibility and biodegradation of 14C-phenanthrene and 14C-octacosane in two soils from former oil refinery facilities over 341 days. The impact of biostimulation and bioaugmentation treatments was also evaluated. At 0, 31, 62, 124 and 341 days, the loss and extractability (using dichloromethane, methanol:water and hydroxypropyl-β-cyclodextrin (HPCD)) of the 14C-hydrocarbons were measured. Further at each time point, the mineralisation of the 14C-hydrocarbons was measured respirometrically under the different conditions. In general, extractions with methanol: water and HPCD were similar for both hydrocarbons in the different treatments; however, these values were less that those measured with DCM. Overall, significantly higher (p ≤ 0.05) amounts of 14C-phenanthrene were lost, readily extracted and mineralised in the soils, with treatments having little impact upon the degradation of this hydrocarbon over 341 days. Conversely, bioaugmentation significantly increased the loss of 14C-octacosane residues from soils and sustained degradation after 31 days. Surprisingly, HPCD and methanol:water both under-predicted the extent to which the contaminants were degraded at each time point. Determining the likelihood of effective biodegradation by the stimulation of indigenous microorganisms or through bioaugmentation needs to be assessed by both chemical and biological measurements of bioaccessibility, rather than just by that which is totally extractable from soil. However, soils which have high loadings of organic matter and/or organic contaminants may prevent accurate assessment of contaminant bioaccessibility, as measured by HPCD.

IMPROVEMENT AND ESTIMATION OF ORALLY DISINTEGRATING TABLETS CONTAINING PILOCARPINE 2-HYDROXY PROPYL β-CYCLODEXTRIN INCLUSION COMPLEX BY RESPONSE SURFACE METHODOLOGY

Objective: The study aimed to develop and evaluate an orally disintegrating tablet that contains pilocarpine and 2-hydroxy propyl β-cyclodextrin as an inclusion complex that is prepared by lyophilization used for treatment for dry mouth. Pilocarpine is utilized to treat dry mouth disorder. The inclusion complex lowers the taste of pilocarpine through the oral mucosa by the use of 2-hydroxy propyl β-cyclodextrin.
 Methods: The in vitro release from the insertion complex is also been studied. The parameters like differential scanning calorimetry (DSC), Fourier transformer infrared spectroscopy (FTIR), X-ray diffraction (XRD), and morphological study have been evaluated. The design of an experiment is carried out based on the concentration of croscarmellose sodium (CCS) and microcrystalline cellulose (MCC). Evaluation of the prepared orally disintegrating tablets have been carried out by different test methods like weight variation, thickness, drug content, disintegration, and in vitro dissolution study.
 Results: Orally disintegrating tablets are studied by utilizing the immediate pressure technique. Pilocarpine indicates the anhydrous crystalline medication, displaying sharp endothermic top at 120.2 °C, bend of 2-HPβCD demonstrates an exceptionally wide endothermal wonder among 55-100 °C for DSC. In pilocarpine spectra, characteristic band of aromatic C-H stretch at 3277 cm-1, C=C stretching at 1608 cm-1, C-N stretching at 1445 cm-1 and methoxy (CH3-O-) stretch at 2921 cm-1 was observed. The investigation shows that tablet hardness of 4.3N, breaking downtime of 12 sec and mean disintegration time is 1.562 min.
 Conclusion: The different diluents and super disintegrating have been applied for the quick elevation of dry mouth that helps us for patient compliance.