دسترسی یکساله به بیش از ۵۰۰ ژورنال روز جهان موجود در سامانه
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Mesoporous Silica Carrier-Based Composites for Taste-Masking of Bitter Drug: Fabrication and Palatability Evaluation
doi : 10.1208/s12249-022-02227-7
23, Article number: 75 (2022)
Abstract. Palatability is one of the most critical characteristics of oral preparations. Therefore, the exploration of new techniques to mask the aversive taste of drugs is in continuous demand. In this study, we fabricated and characterized composites based on mesoporous silica (MPS) that consisted of MPS, a bitter drug, and release regulators. We conducted a palatability evaluation to assess the taste-masking efficacy of the composites. The composites were prepared using the dry impregnation method combined with hot-melt extrusion. Morphology and components distribution in composites were characterized by scanning electron microscopy, confocal laser scanning microscopy, X-ray photoelectron spectroscopy, powder flow properties evaluation, and nitrogen-sorption measurement. The results demonstrated that drugs mainly existed in the inner pore of composites, and release regulators existed in the inner pore and covered the composites’ surface. Interactions among the composite components were studied using powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. The drug loaded into the composites was amorphous, and an intermolecular interaction occurred between the drug and the MPS. Taste-masked composites significantly reduced drug release levels under mouth conditions; thus, they prevented the interaction of the dissolved drug with taste receptors and improved palatability. An electronic tongue evaluation and a human taste panel assessment confirmed the better palatability of taste-masked composites. Moreover, the desired drug release behavior can be adjusted by choosing an appropriate release regulator, with stronger hydrophobicity of release regulators resulting in slower drug release. This work has provided new insights into taste-masking strategies for drugs with unpleasant tastes.
Donepezil HCl Liposomes: Development, Characterization, Cytotoxicity, and Pharmacokinetic Study
doi : 10.1208/s12249-022-02209-9
23, Article number: 74 (2022)
The current research work aims to study the pharmacokinetic and nasal ciliotoxicity of donepezil liposome–based in situ gel to treat Alzheimer’s disease. The physicochemical properties and first-pass metabolism of donepezil HCl result in low concentrations reaching the brain post oral administration. To overcome this problem, donepezil HCl–loaded liposomes were formulated using the ethanol injection method. The donepezil HCl–loaded liposomes were spherical with a size of 103 ± 6.2 nm, polydispersity index of 0.108 ± 0.008, and entrapment efficiency of 93 ± 5.33 %. The optimized in situ gel with donepezil HCl–loaded liposomes showed 80.11 ± 7.77 % drug permeation than donepezil HCl solution–based in situ gel (13.12 ± 4.84 %) across sheep nasal mucosa. The nasal ciliotoxicity study indicated the safety of developed formulation for administration via nasal route. The pharmacokinetics and biodistribution study of developed formulation showed higher drug concentration (1239.61 ± 123.60 pg/g) in the brain after nasal administration indicating its better potential via the nasal pathway. To treat Alzheimer’s disease, the administration of liposome-based in situ gel through the nasal pathway can therefore be considered as an effective and promising mode of drug delivery.
In Vitro Assessment of Sunscreen Efficacy Using Fourier Transform Infrared (FTIR) Spectroscopy on Synthetic Skin
doi : 10.1208/s12249-022-02224-w
23, Article number: 73 (2022)
Although there are several methods for assessing the sun protection factor (SPF) of sunscreen products, there is no standard and reliable in vitro method. Each test entails limitations and drawbacks. Therefore, this study aimed to assess the employability of FTIR as an alternative and quick method to evaluate the efficacy of various sunscreen formulations, their concentrations, and the timing of their application. Infrared radiation has longer wavelengths than ultraviolet, penetrates deeply into the skin, and hence enables the understanding of sunscreens’ ability to block the transmission of radiation. The FTIR transmission using synthetic skin to study the effect of sunscreen agents (oxybenzone, octyl methoxycinnamate, titanium dioxide (TiO2), and zinc oxide (ZnO)) was conducted in the range 450–4000cm−1. Comparison studies were made at the peak of 805cm−1. After 2 h of sunscreen application, using the maximum concentrations, the FTIR peak at wavenumber 805cm−1 demonstrated a significant reduction of transmission from 96.55 to 60.09%, 57.59%, 32.02%, and 37.1% for oxybenzone, octyl methoxycinnamate, TiO2, and ZnO respectively (P<0.05). A significant reduction in transmission was observed (P<0.05) with increasing sunscreen concentrations after 2 h of application. Nevertheless, the upper limit of concentration showed no appreciable change from the middle level of concentration, and hence it is cost-effective to employ the middle concentration. Inorganic sunscreens showed a higher protection level than organic. Fixed-dose combinations of sunscreens showed an enhanced effect yet were not synergistic. In conclusion, the use of FTIR spectroscopy with synthetic skin is a quick and user-friendly technique that enables the assessment of the efficacy of sunscreen formulations.
Microwave-Assisted Physically Cross-Linked Chitosan-Sodium Alginate Hydrogel Membrane Doped with Curcumin as a Novel Wound Healing Platform
doi : 10.1208/s12249-022-02222-y
23, Article number: 72 (2022)
This project purposes to develop chitosan and sodium alginate–based hydrogel membranes loaded with curcumin through microwave-based physical cross-linking technique and its evaluation for wound healing potential. For the purpose, curcumin-loaded chitosan and sodium alginate membranes were developed using microwave at fixed frequency of 2450 MHz, power 350 W for 60 s, and tested for their physicochemical attributes like swelling, erosion, surface morphology, drug content, and in vitro drug release. The membranes were also subjected to tensile strength and vibrational and thermal analysis followed by testing in vivo on animals. The results indicated that microwave treatment significantly enhanced the swelling ability, reduced the erosion, and ensured smooth surface texture with optimal drug content. The drug was released in a slow fashion releasing total of 41 ± 4.2% within 24-h period with a higher tensile strength of 16.4 ± 5.3 Mpa. The vibrational analysis results revealed significant fluidization of hydrophilic domains and defluidization of hydrophobic domains which translated into a significant rise in the melting temperature and corresponding enthalpy which were found to be 285.2 ± 3.2 °C and 4.89 ± 1.4 J/g. The in vivo testing revealed higher percent re-epithelialization (75 ± 2.3%) within 14 days of the treatment application in comparison to only gauze and other treatments applied, with higher extent of collagen deposition having well-defined epidermis and stratum corneum formation. The microwave-treated chitosan-sodium alginate hydrogel membranes loaded with curcumin may prove to be another alternative to treat skin injuries.
Formulation of Apigenin-Cyclodextrin-Chitosan Ternary Complex: Physicochemical Characterization, In Vitro and In Vivo Studies
doi : 10.1208/s12249-022-02218-8
23, Article number: 71 (2022)
The current investigation was performed with an aim to improve the aqueous solubility, dissolution rate, and thus the biological activity of apigenin (APG) using the solubilizers hydroxypropyl beta-cyclodextrin (HPβCD) and chitosan (CTSN). A binary and ternary inclusion complexes of APG with HPβCD and CTSN were prepared by physical mixing, fusion, and solvent evaporation methods. The liquid state characterization of the APG, the solubilizers, and the physical and chemical interactions between them was done through phase solubility approach. The solid-state characterization was performed by proton nuclear magnetic resonance (1H-NMR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD). The in vitro dissolution test and antioxidant activity and in vivo anti-inflammatory activity of the ternary inclusion complex in albino rats were performed to assess the performance of the APG. Phase solubility study results revealed a remarkable increase in apparent stability constant (Kc) and complexation efficiency (CE) of HPβCD in presence of CTSN in ternary complex with above 8 folds more increment in solubility of APG than its binary complex. The in vitro dissolution rate, antioxidant activity, and the anti-inflammatory effect of the APG ternary inclusion complex were found to be significantly higher than that of pure APG. Solid state characterization confirmed the formation of a ternary inclusion complex. 1H-NMR study gave more insight at molecular level into how different groups of APG were responsible for complex formation with the HPβCD and how CTSN was significantly influencing on the APG-HPβCD complex formed. Nevertheless, pharmacokinetic and histopathological studies of our APG-HPβCD-CTSN ternary complex would yield much rewarding results.
Transfersome Hydrogel Containing 5-Fluorouracil and Etodolac Combination for Synergistic Oral Cancer Treatment
doi : 10.1208/s12249-022-02221-z
23, Article number: 70 (2022)
Oral cancer is one of the most common malignancies with an increased rate of incidence. 5-Fluorouracil (5FU) is an effective chemotherapeutic indicated for oral cancer treatment. Etodolac (Et), a cyclooxygenase-2 inhibitor, can be used as an adjuvant agent to sensitize cancer cells to chemotherapy. The aim of this work was to prepare and characterize 5FU and Et dual drug–loaded transfersomes to treat oral cancer. Transfersomes were prepared by thin-film hydration method and characterized for the average particle size and zeta-potential using dynamic light scattering and scanning electron microscopy techniques. The prepared transfersomes were further characterized for their drug loading, entrapment efficiencies using amicon centrifuge tubes and drug release behavior using cellulose membrane. The synergistic activity of dual drug–loaded transfersomes was studied in FaDu oral cancer cells. Results showed that the average particle size, polydispersity index, and zeta potential were 91±6.4 nm, 0.28±0.03, and (−)46.9±9.5 mV, respectively, for 5FU- and Et (1:1)-loaded transfersomes. The highest encapsulation efficiency achieved was 36.9±3.8% and 79.8±6.4% for 5FU and Et (1:1), respectively. Growth inhibition studies in FaDu cells using different concentrations of 5FU and Et showed a combination index of 0.36, indicating a synergistic effect. The FaDu cell uptake of drug-loaded transfersomes was significantly (p<0.05) greater than that of free drugs. The transfersome hydrogel made of HPMC (2% w/w) showed similar flux, lag time, and permeation coefficient as that of drug-loaded transfersomes across excised porcine buccal tissue. In conclusion, 5FU and Et transfersome hydrogel can be developed for localized delivery to treat oral cancer.
Investigation of Chloroquine Resinate Feasibility and In Vitro Taste Masking Evaluation for Pediatric Formulations
doi : 10.1208/s12249-022-02219-7
23, Article number: 69 (2022)
In this study, chloroquine resinates were prepared at a 1:1 (w:w) drug-to-resin ratio using the batch method with polacrilex (PC), sodium polystyrene sulfonate (SPS), and polacrilin potassium (PP) ion exchange resins (IER). The influence of drug/resin ratio and pH of the medium on drug loading efficiency was explored. UV-VIS spectrophotometric analysis showed that SPS resin had high loading efficiency for chloroquine diphosphate (CLP), above 89%, regardless of the pH. PP resin was more effective at pH 5.0 (90.68%) than at pH 1.0 (2.09%), and PC resin had only 27.63% of CLP loading efficiency. CLP complexation with IER yielded amorphous mixtures according to results from differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD), thus indicating drug-resin interaction. The taste masking efficiency was evaluated with in vitro methods using an adapted dissolution test and an electronic tongue system. During dissolution tests, SPS released only 1.0% of CLP after 300 s, while PP released over 10% after 90 s in simulated saliva solution. The electronic tongue distinguished the samples containing CLP, resins, and resinates by using multidimensional projection techniques that indicated an effective drug taste masking. In an accelerated stability study, the drug contents did not decrease in chloroquine resinates, and there was no physical degradation of the resinates after 60 days. Using chloroquine resinates therefore represents a novel way to evaluate taste masking in vitro which is relevant for the early formulation development process.
Improving Water-Absorption and Mechanical Strength: Lyotropic Liquid Crystalline–Based Spray Dressings as a Candidate Wound Management System
doi : 10.1208/s12249-021-02205-5
23, Article number: 68 (2022)
A spray dressing based on lyotropic liquid crystalline (LLC) with adjustable crystalline lattices was investigated in this study. It possesses water-triggering phase transition property and ease of spraying on wound, as well as stable drug encapsulation and controllable drug release. When it comes to wound with exudate, adequate water absorption and sustainable mechanical strength after water absorption was important for a good dressing, while most of the normal LLC dressings were still unable to meet such standards. Herein, a type of hyaluronic acid (HA)–incorporated LLC-based spray dressing (HLCSD) was developed to overcome the above limitations. After comparing HAs with different molecular weights (MWs) and concentrations, 3% HA with MW of 800~1000 kD was chosen as an ideal amount of excipients to add into the HLCSD. The water absorption of HLCSD precursor increased by 150% with the appearance of enlarged water channels. The complex modulus of HLCSD gel also increased from 1 to 100 kPa, which suggested lasting wound coverage and good patient compliance when used clinically. The spraying and phase transition properties of HLCSD was studied and showed acceptable changes. Moreover, good safety comparable with the commercial product Purilon® was also demonstrated in an in vivo acute skin irritation test. Thus, the improved HLCSD was a promising dressing for exudation wound treatment.
