Hydroxypropyl Β-cyclodextrin Research Articles

Quantifying the hygroscopic properties of cyclodextrin containing aerosol for drug delivery to the lungs.

Aerosol dynamics is important to quantify in drug delivery to the lungs with the aim of delivering therapeutics to a target location and optimising drug efficacy. The macrocycle (2-hydroxypropyl)-β-cyclodextrin (2-HP-β-CD) is thought to alleviate symptoms associated with neurodegenerative diseases when inhaled but the hygroscopic response is not well understood. Here we measure the hygroscopic growth of individual aqueous aerosol containing 2-HP-β-CD in optical tweezers through analysis of morphology-dependent resonances arising in Raman spectra. Droplets are analysed in the size range of 3-5 μm in radius. The evolving radius and refractive index of each droplet are measured in response to change in relative humidity from 98-20% to determine mass and radius based hygroscopic growth factors, and compared with dynamic vapour sorption measurements. Bulk solution refractive index and density measurements were used in accordance with the self-consistent Lorenz-Lorentz rule to determine melt solute and droplet properties. The refractive index of 2-HP-β-CD was determined to be 1.520 ± 0.002 with a density of 1.389 ± 0.005 g cm-3. To our knowledge, we show the first aerosol measurements of 2-HP-β-CD and determine hygroscopicity. By quantifying the hygroscopic growth and physicochemical properties of 2-HP-β-CD, the impact of aerosol dynamics can be accounted for in tailoring drug formulations and informing models used to predict drug deposition patterns within the respiratory system.

Use of hydroxypropyl β-cyclodextrin as a dual functional component in xanthan hydrogel for sustained drug release and antibacterial activity

A hydrogel of xanthan gum (XG) was improved by crosslinking hydroxypropyl β-cyclodextrin (HPCD) physically to construct a novel drug delivery system. This hydrogel was full of the textures due to directional self-aggregations of XG helixes observed by optical microscopy and scanning electron microscopy. Rheological measurements indicated that HPCD added into XG hydrogel affected the dynamic behaviors of the hydrogel system, and the melting point of the hydrogels also rose from 117.5 °C up to 125.8 °C due to the enhancement of the supramolecular interactions. The XG/HPCD hydrogel with mass ratios 4:3 presented more elastic network than other XG/HPCD hydrogels did, which was more suitable for drug delivery. The supramolecular interactions in the gel network were mainly hydrogen bonding by the results of Fourier transform infrared spectroscopy. X-ray powder diffraction showed the XG/HPCD xerogel with amorphous characters to the benefit of loading drugs. The drug hydrogel loading anticancer methotrexate performed an effective controlled release, reflecting a host of HPCD molecule enhanced binding of drug methotrexate. And the hydrogel loading levofloxacin also exhibited fair antibacterial effects with inhibition zone method. Hence, this XG/HPCD hydrogel obtained would be a novel and interesting drug delivery system indeed.

Formulation and Evaluation of Cyclodextrin-Based Thermosensitive In Situ Gel of Azithromycin for Periodontal Delivery

This study aims to formulate and evaluate the temperature-sensitive in situ gel of 0.5% (w/v) azithromycin (AZM) containing cyclodextrin inclusion complex by the cold method. To increase its aqueous solubility, it was incorporated as an inclusion complex in a 1:1 M ratio with hydroxypropyl β-cyclodextrin (HPβ-CD). The central composite design was used to optimize the effect of poloxamer 407 and Carbopol 934P (independent factors) on dependent factors such as percentage drug release at first hour (t50% and t90%), gelation temperature, and viscosity. Both the independent factors had a significant effect on the entire five response factors (p < 0.05). Each formulation was evaluated for clarity, pH, spreadability, syringeability, gelation strength, mucoadhesive property, in vitro drug release, gelation temperature, viscosity, and rheology. Based on maximum desirability, formulation containing 18.91% (w/v) of poloxamer 407 and 0.353% (w/v) of Carbopol 934P was considered an optimized batch. The value of percentage relative error exhibited a close agreement between observed and predicted values calculated using regression equations. Further, the optimized formulation showed a good drug release for a period of 54 h, which was more effective in the treatment of periodontal disease. Thus, azithromycin (AZM) can be successfully formulated as a thermosensitive in situ mucoadhesive gel containing HPβ-CD for periodontal drug delivery.

NANO-SPONGE NOVEL DRUG DELIVERY SYSTEM AS CARRIER OF ANTI-HYPERTENSIVE DRUG

Objective: The study was designed to prepare Nano-sponge formulation loaded with nifedipine. Studying parameters which affecting the formulas in addition to pharmacokinetics and toxicity tests.&#x0D; Methods: Nine Nano-sponge formulations were prepared by the solvent evaporation technique. Different ratios of polymer ethylcellulose, CO-polymers β-cyclodextrin and hydroxypropyl β-cyclodextrin in addition to solubilizing agent polyvinyl alcohol were used. Thermal analysis, X-ray powder diffraction (XRPD), shape and surface morphology, particle size, %production yield, %porosity, % swelling, and % drug entrapment efficiency of Nano-sponge were examined. Release kinetic also studied beside comparison of pharmacokinetic parameters of the optimum choice formula and marketed one in addition to Toxicological consideration.&#x0D; Results: Particle size in the range of 119.1 nm to 529 nm which were increased due to the increase in the concentration of polymer to the drug. Nano-sponge revealed porous, spherical nature. Increased in the drug/polymer molar ratios (1:1 to 1:3) may increase their % production yield ranged from 62.1% to 92.4%. The drug content of different formulations was in the range of 77.9% to 94.7%, and entrapment efficiency was in the range of 82.72 % to 96.63%. Drug released in controlled sustained pattern and followed Higuchi, s diffusion mechanism. Pharmacokinetic parameters of optimized formula showed significant higher maximum plasma drug concentration, area under plasma concentration-time curve, volume of distribution and mean residence time. Nano-sponge loaded drug proved biological safety at low concentrations.&#x0D; Conclusion: Nano-sponge drug delivery system has showed small Nano size, porous with controlled drug release and significant-high plasma drug concentration that improved solubility, drug bioavailability and proved safety.

Polydopamine-coated polyethylene sieve plate as an efficient and convenient adsorption sink for the bioaccessibility prediction of PAHs in soils

Bioaccessibility measurements of polycyclic aromatic hydrocarbons (PAHs) in soils are significant for exposure risk assessment. The current physicochemical methods require tedious operation processes, underestimate the actual risks, or are unsuitable for high organic content soils. In this work, an efficient and convenient method based on polydopamine-coated polyethylene sieve plate (PDA@PESP) and hydroxypropyl-β-cyclodextrin (HPCD) was developed to predict the bioaccessibility of PAHs in multi-type soils. The PDA@PESP can be prepared via in situ self-polymerization, allowing to extract PAHs from HPCD solution quantitatively and rapidly. When applied to evaluate the bioaccessibility with PDA@PESP as an adsorption sink and HPCD as a diffusive carrier, the proposed method can significantly improve the extractable fraction of PAHs compared to single HPCD extraction in particular for high organic carbon content soil and high-ring PAHs. The desorption kinetics data indicated that the method can predict the bioaccessible fraction of PAHs. In addition, the method predicted a satisfactory accumulation into earthworms (Eisenia fetida) with a slope statistically approximated to 1. A highly significant linear regression (R2 = 0.95) was also found between the proposed method and Tenax desorption in historically contaminated soils, demonstrating that the method is an efficient and convenient approach for the bioaccessibility prediction of PAHs in soils.

Differential Properties of Nanoporous Nanosponges Prepared from β-Cyclodextrin and 2-Hydroxypropyl β-Cyclodextrin

Differential Properties of Nanoporous Nanosponges Prepared from <i>β</i>-Cyclodextrin and 2-Hydroxypropyl <i>β</i>-Cyclodextrin

Angiotensin-(1-7) oral treatment after experimental myocardial infarction leads to downregulation of CXCR4

Myocardial infarction triggers cellular events that starts with the activation of inflammatory response and fibrogenic pathways involved in cardiac tissue remodeling. Angiotensin-(1–7) (Ang-(1–7)) is an endogenous heptapeptide from the renin-angiotensin system with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Although the beneficial aspects of Ang-(1–7) in animal models of cardiac ischemia have been reported, the molecular events underlying Ang-(1–7) cardioprotective effect remains elusive. This study investigated the impact of oral treatment with Ang-(1–7) included in hydroxypropyl β-cyclodextrin (HPβCD/Ang-(1–7)) on the cardiac proteome dysregulation due to experimental myocardial infarction. Wistar male rats were submitted to experimental myocardial infarction and treated daily with HPβCD/Ang-(1–7) during 7 days or 60 days by gavage. Our results showed that HPβCD/Ang-(1–7) treatment ameliorates the post-infarction condition due to the modulation of proteins that initially favor the resolution of inflammation and mitochondrial dysfunction. Moreover, this study reported for the first time that Ang-(1–7) treatment after experimental myocardial infarction leads to the downregulation of the C-X-C chemokine receptor type 4 (CXCR4). SignificanceMyocardial infarction triggers a sequence of cellular and molecular events that starts with an intense inflammatory response that is resolved in the proliferative phase. Prolonged inflammatory phase can lead to adverse cardiac repair and heart failure. In this context, we proposed a post-MI treatment using Ang-(1–7) included in HPβCD and administrated orally. We observed that HPβCD/Ang-(1–7) treatment led to CXCR4 downregulation, highlighting this C-X-C chemokine receptor as a potential therapeutic target for ischemic heart diseases.

Interaction with Modified Cyclodextrin as a Way to Increase the Antimalarial Activity of Primaquine.

Malaria is still a dangerous disease that impacts specifically Africa, Asia, and Latin America. The development of therapies to overcome the parasite infection is an important challenge nowadays. The medicine primaquine (PQ) is used in the treatment, although several side effects and low oral bioavailability are reported. This work focused on the preparation and characterization of a complex between PQ and 2- hydroxypropyl-β-cyclodextrin (HPCD), besides performing release tests of this formulation. PQ:HPCD complexes were prepared at 1:1 and 1:2 molar ratios, by the lyophilization method. The association between PQ and HPCD was tested using UV-vis, infrared (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy and NMR techniques (chemical shift, Job Plot, DOSY, and ROESY). Tests were also conducted to evaluate drug release before and after complexation with HPCD. Results showed that there was a weak interaction of PQ with HPCD, forming non-inclusion complexes. These results were supported by FTIR results and spatial correlations between hydrogens from PQ with the external HPCD hydrogens. A 1:2 PQ:HPCD preferred molar ratio was determined by DSC and Job Plot experiments and the time to release 96% of the drug was 21.2 h slower after complexation. Conclusion indicate that PQ interacts poorly with HPCD, probably due to its hydrophilic character, as well as to its interaction with the external rim of HPCD. Our results demonstrate that there was a significant improvement in the release time after the complexation process, which could lead to an increase in the activity of the drug.

Complexation and physicochemical analysis of hydrophobic molecules of methyl jasmonate with Hydroxypropyl-β–Cyclodextrin

In the present study, methyl jasmonate (MeJa) was included in 2-hydroxypropyl-β-cyclodextrin (HPβCD) by grinding (M1), freeze drying (M2), co-precipitation + freeze drying (M3) and by applying supercritical carbon dioxide (M4). FT-IR/ATR, FT-Raman, TGA, and DSC analyses of the complexation products confirmed that MeJa/HPβCD complexes were formed by the four different examined methods of inclusion. FT-IR/ATR supported the inclusion, mainly based on the reduction of intensity of absorption at the wavelength of maximum absorbance of free MeJa (1733 cm-1), which was 27.69 au before inclusion. From these results, M3 (2.29 au) and M4 (0.90 au) were the most efficient techniques for complexation. TGA, and DSC analyses pointed out that the complexes formed by the methods M3 and M4 had the least loss of mass below approximately 305°C (the temperature that free HPβCD starts to decompose thermally). Except for M1, the results of antioxidant activity (AA) based on the DPPH assay revealed that the AA of the inclusion compounds were higher than that of free MeJa (α = 0.05). The best methods in terms of AA and thermal stability of the formed inclusion compounds were M3 and M4.

Molecular Encapsulation of Eucalyptus staigeriana Essential Oil by Forming Inclusion Complexes with Hydroxypropyl-β-Cyclodextrin

This study investigated the inclusion complex of Eucalyptus staigeriana essential oil (ESEO) formed with hydroxypropyl-β-cyclodextrin (HPCD) as a model system to determine which essential oil (EO) components were encapsulated in the complex. The ESEO/HPCD inclusion complex was prepared in aqueous solution and consequently analyzed by gas chromatography-mass spectrography (GC-MS), ultraviolet–visible spectroscopy (UV-VIS), thermogravimetric–differential thermal analysis (TG-DTA), 1H ROESY NMR, and molecular modeling. The results clearly showed that inclusion complexes had been successfully formed between ESEO and HPCD. It was demonstrated that the EO components did not form an inclusion complex with HPCD in equal proportions, but certain EO components were preferentially encapsulated. Components such as alcohols and aldehydes were preferentially encapsulated by HPCD, leading to higher concentrations of these compounds in the complex. This implies that encapsulation of EOs by forming inclusion complexes with HPCD may alter their composition in the complexes with potential changes in their properties such as antimicrobial activity.

A Spectroscopic Study of Solid-Phase Chitosan/Cyclodextrin-Based Electrospun Fibers

In this study, chitosan (chi)/hydroxypropyl-β-cyclodextrin (HPCD) 2:20 and 2:50 Chi:HPCD fibers were assembled via an electrospinning process that contained a mixture of chitosan and HPCD with trifluoroacetic acid (TFA) as a solvent. Complementary thermal analysis (thermal gravimetric analysis (TGA)/differential scanning calorimetry (DSC)) and spectroscopic methods (Raman/IR/NMR) were used to evaluate the structure and composition of the fiber assemblies. This study highlights the multifunctional role of TFA as a solvent, proton donor and electrostatically bound pendant group to chitosan, where the formation of a ternary complex occurs via supramolecular host–guest interactions. This work contributes further insight on the formation and stability of such ternary (chitosan + HPCD + solvent) electrospun fibers and their potential utility as “smart” fiber coatings for advanced applications.

The Effect of Carrier Matrix and the Method of Preparing Solid Dispersion on Physical State and Solubility of Ibuprofen

Background: The poor solubility of a drug substance is one of the factors which are responsible for poor dissolution and bioavailabity. Objective: To enhance the solubility of Ibuprofen using different techniques, and to investigate the effect of carrier matrixes and methods of preparing solid dispersion on physical state and solubility of Ibuprofen. Methods: Fusion method, solvent evaporation and effervescence assisted fusion methods were used to prepare solid dispersions of ibuprofen (IBU). Mannitol, polyethylene-glycol-6000, urea, microcrystalline cellulose, calcium carbonate, sugar spheres, sodium chloride, magnesium oxide, titanium dioxide, citric acid, hydroxypropyl-β-cyclodextrin and β-cyclodextrin were used as carrier matrix. Solid dispersions were characterized using scanning electron microscopy and Differential Scanning Calorimetry (DSC). The solubility of IBU powder and its solid dispersions were investigated in water, acidic buffer (pH-1.2) and in phosphate buffer (pH-6.8). Results: In some of the solid dispersions, IBU lost its crystalline structure and converted into amorphous powder. Scanning electron micrographs and DSC thermograms revealed the absence of IBU crystalline particles in few of the solid dispersion matrixes. Solid dispersion comprising amorphous IBU showed remarkable enhancement in its solubility. The IBU-magnesium oxide solid dispersion showed the highest solubility enhancement, followed by IBU-hydroxypropyl-β-cyclodextrin, IBUpolyethylene glycol-6000, IBU-urea and IBU-β-cyclodextrin. The magnesium oxide, hydroxypropyl-β- cyclodextrin and β-cyclodextrin enhanced solubility even at acidic pH. Effervescence assisted fusion technique showed better solubility results than the other two techniques. Conclusions: On the basis of present observations, it can be suggested that the type of carrier matrix, the method of preparation and the pH of the dispersion plays an important role in the solubility of IBU.

Preparation, Characterization, and In vitro Evaluation of Curcumin- and Resveratrol-Loaded Solid Lipid Nanoparticles.

Curcumin and resveratrol are natural compounds with significant anticancer activity; however, their bioavailability is limited due to poor solubility. This study aimed to overcome the solubility problem by means of solid lipid nanoparticles (SLN). 2-Hydroxypropyl β-cyclodextrin (HPβCD) was selected from a range of polymers based on miscibility and molecular interactions. SLNs were obtained by probe sonication and freeze-drying curcumin-resveratrol with/without HPβCD incorporated in gelucire 50/13. SLNs were characterized by dynamic light scattering (DLS), zeta potential, powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), and physical stability. The in vitro release of drugs from the SLNs was performed by the direct dispersion method and analyzed using a validated UV-visible method. In vitro efficacy was tested using a colorectal cancer cell line. Curcumin-resveratrol-gelucire 50/13-HPβCD (CRG-CD) and curcumin-resveratrol-gelucire 50/13(CRG) SLNs showed a particle size from 100 to 150nm and were not in thecrystalline state per PXRD results. MDSC results complimented PXRD results by theabsence of melting endotherm of curcumin; TGA showed no weight loss, confirming theabsence of organic solvent residual, and the shape of the SLNs was confirmed as spherical by SEM. CRG SLNs were stable for 21days with respect to particle size and zeta potential. MTT assay indicated better IC50 value for CRG as compared to CRG-CD. Hence, novel SLNs of curcumin and resveratrol incorporated in gelucire 50/13 and HPβCD were prepared and characterized to improve their bioavailability and anticancer activity.

Enhancement of Dissolution of Fenofibrate Using Complexation with Hydroxy Propyl β-Cyclodextrin

The aim of the present study was to enhance the dissolution rate of fenofibrate using complexation with hydroxy propyl β-cyclodextrin (HPβCD). The phase solubility behavior of fenofibrate was studied in various concentrations of (HPβCD) aq. solution at 37°C. The solubility of fenofibrate increased with an increase in the amount of HPβCD aq. solution. Gibbs free energy (ΔG°)tr values were all negative. Complexes of fenofibrate with HPβCD were prepared in 1:1 ratio by kneading and coprecipitation. These complexes were evaluated by dissolution studies, fourier transform infrared (FTIR) spectroscopy, and differential scanning calorimetry (DSC) studies. The complexation of fenofibrate with HPβCD exhibited an enhanced dissolution rate. The mean dissolution time of fenofibrate decreased significantly upon complexation. FTIR studies showed the formation of intermolecular hydrogen bonding between fenofibrate and HPβCD. DSC studies indicated a loss in crystalline state of fenofibrate in complexes. Complexation with HPβCD can be used as a useful tool for the enhancement of dissolution of fenofibrate.

Consciousness Energy Healing Treatment: Spectroscopic and Calorimetric Evaluation of the Biofield Energy Treated Hydroxypropyl β-Cyclodextrin

Hydroxypropyl β-Cyclodextrin (HPBCD) used in food, pharmaceutical, chemical industries, as well as environmental, and agriculture engineering. But the major issue related to HPBCD is the low solubility profile. In this study, the influence of the Consciousness Energy Healing Treatment (the Trivedi Effect®) on the physicochemical properties of HPBCD was evaluated using spectroscopic and calorimetric analytical techniques. The test sample (HPBCD) was divided into control sample and treated sample. The control sample did not receive the Biofield Energy Treatment. Whereas, the treated sample received the Biofield Energy Treatment remotely by a renowned Biofield Energy Healer, Dahryn Trivedi. The particle size values of the treated sample were decreased by 3.28%(d10), 1.36%(d50), 0.45%(d90), and 1.04%{D(4,3)}; therefore, the specific surface area was increased by 1.9% compared with the control sample. The evaporation temperature of the treated HPBCD sample was significantly decreased by 19.89%; however, the latent heat of evaporation and latent heat of fusion were significantly increased by 56.27% and 47.41%, respectively compared with the control sample.The total weight loss in the treated HPBCD was decreased by 5.11%; whereas, the residue amount was significantly 309.67% more compared to the control sample.The results indicated that the Trivedi Effect® might have produced a new form of HPBCD which may show better thermal stability, solubility, dissolution rate, and bioavailability. This new form of HPBCD would be more useful for improvement of solubility of the lipophilic drug, preparation of cholesterol free food products, weight loss supplements, anti-obesity medication, stabilize volatile and unstable compounds, and other manufacturing industry using it as a raw material.

Inclusion Complex of 2-Methyl Mercapto Phenothiazine with Hydroxy Propyl β-Cyclodextrin: Characterization and Cytotoxic Activity Evaluation

Abstract A host-guest inclusion complex of hydroxy propyl β-cyclodextrin (HBCD) and 2-methyl mercapto phenothiazine (2MMPT) was prepared and investigated in liquid state and in solid state. In liquid state, UV-visible and fluorescence spectroscopic methods are used to investigate the inclusion complex. The binding constant of 2MMPT: HBCD inclusion complex was calculated using Benesi-Hildebrand plot. The 1:1 stoichiometric ratio of inclusion complex was derived from Benesi-Hildebrand plot and Job’s plot of continuous variation method. The solid HBCD: 2MMPT inclusion complex was prepared by coprecipitation method and characterized using FT-IR, 1 H NMR, 13 C NMR, and ESI-MS analytical methods. The cytotoxicity of HBCD: 2MMPT inclusion complex was studied on human breast cancer cell line MCF 7 showed that the cell cytotoxicity of HBCD: 2MMPT inclusion complex was close to free 2MMPT and inclusion complexation with HBCD retained the anticancer activity of 2MMPT.

Physicochemical characterization and antibacterial activity assessment of lavender essential oil encapsulated in hydroxypropyl-beta-cyclodextrin

Lavender essential oil (LEO) is a natural antimicrobial agent, but its poor aqueous solubility and high volatility limit its application in food systems. Cyclodextrin is a useful embedding material for active compounds and can protect their bioactivity and structural integrity. Therefore, the aim of this paper was to investigate the physicochemical properties and antibacterial activities of the LEO encapsulated in hydroxypropyl-β-cyclodextrin (HPCD). Changes in the constituent of the LEO after forming a composite with HPCD were identified via gas chromatography-mass spectrometry (GC–MS) analysis in comparison with pure LEO. Linalyl anthranilate and linalool were the major components in the LEO; however, their relative contents changed dramatically after encapsulating with HPCD. Molecular modelling of the major ingredients (i.e., linalyl anthranilate and linalool) and their HPCD composites was performed using a PM3 method to explain the binding behaviour and the host/guest geometry. In the antibacterial activity tests, the MIC of the LEO could be increased approximately 3-fold against Staphylococcus aureus, Escherichia coli and Candida albicans after encapsulation in HPCD. These results suggested that the change in constituents of the LEO had a significant impact on the stability and antibacterial activity of LEO. This composite might be a potential antimicrobial for inhibiting pathogens in food systems.

Effect of hydroxypropyl-β-cyclodextrin on the cometabolism of phenol and phenanthrene by a novel Chryseobacterium sp.

Cometabolic degradation is an effective method to remove the polycyclic aromatic hydrocarbons (PAHs) with phenol as growth substrate from coal chemical wastewater (CCW). Unfortunately, the toxicity and low solubility of PAHs always restrict their degradation. In this study, Chryseobacterium sp. H202 was firstly isolated from the aerobic segment of CCW. Then, to improve the cometabolic degradation of PAHs, the effects of hydroxypropyl-β-cyclodextrin (HPCD) were investigated. Phenanthrene removal was accelerated in the presence of phenol; however, the degradation of phenol was inhibited because of the toxicity of phenanthrene. Addition of 50 mg/L HPCD accelerated the degradation of phenol and effectively improved the phenanthrene removal rate by about 55%. Inclusion of HPCD appeared to increase the apparent solubility and reduce the toxicity of phenanthrene, thereby improving the cometabolic degradation of phenol and phenanthrene. Therefore, HPCD can enhance the degradation of phenanthrene with phenol as the growth substrate during CCW treatment.

New chemically modified carbon paste sensor for nanomolar concentration measurement of rifampicin in biological and pharmaceutical media

A new carbon paste electrode for rifampicin (RIF) drug was prepared and fully characterized in terms of composition, usable pH range and temperature. The sensor is based on 2-hydroxypropyl β-cyclodextrin as a good ionophore in the carbon paste matrix. The modified electrode showed a Nernstian slope of 59.2 mV/decade over the concentration range of 3.2 × 10−8 to 2.2 × 10−4 M with a limit of detection 2.3 × 10−8 M. The electrode has a short and stable response time of 4 s. The sensor manifested advantages of simple design, low cost, wide concentration range, excellent selectivity to rifampicin, applicable as an indicator electrode and renewability. The sensor was successfully used for determination of rifampicin in tablet and blood serum samples. Temperature dependence of the sensor potential response was examined in the temperature range of 15–55 °C. The sensor showed a very low thermal coefficient within the studied temperature range.

Drug-in-mucoadhesive type film for ocular anti-inflammatory potential of amlodipine: Effect of sulphobutyl-ether-beta-cyclodextrin on permeation and molecular docking characterization.

Mucoadhesive type ocular film has been prepared for studying the anti-inflammatory potential of amlodipine (AML) on carrageenan-induced rabbit model and the effect of sulphobutyl-ether-beta-cyclodextrin on corneal permeation was tested. Hydroxypropyl methylcellulose (HPMC) ocular film was prepared after complexation of amlodipine with β-cyclodextrin, (BCD), hydroxypropyl β-cyclodextrin (HPCD), and sulfobutylether β-cyclodextrin (SBCD). The film without cyclodextrin showed a maximum swelling, and erosion to the highest extent. Both drug release and permeation were highly diffusion controlled and highest improvement was observed with SBCD due to increased dissolution, compared to other formulations with or without cyclodextrin. Highest binding energy and highest extent of amorphization were noticed in the SBCD film formulation. Improved amlodipine release in-vitro and ocular permeation were found by the HPMC film formulation after complexation of the drug with cyclodextrins wherein SBCD exhibited both to the highest extent. Binary and ternary systems molecular docking studies confirmed the lowest energy of binding between amlodipine and BCD compared to HBCD and SBCD. Signs of acute inflammation were mitigated within 2 h of film application in the cul-de-sac. Presence of sulphobutyl-ether β-cyclodextrin in the amlodipine-HPMC film can improve ocular permeation significantly and could be utilized as mucoadhesive type formulation for anti-inflammatory activity.