Experimental study on the reduction of loratadine particle size through confined liquid impinging jets

Emami, M.; Haghshenasfard, Masoud; Zarghami, Reza; Sadeghi, Roohollah; Esfahany, Mohsen Nasr

doi:10.1016/j.ijpharm.2020.119668

Cited by 8 publications

(4 citation statements)

References 36 publications

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“…Prominent pure LORA peaks in 1701, 1643, 1440, 1228, 1095, and 999 cm −1 , corresponding to the C = O, C = N, C = C, C–N, C–Cl, and = C–H vibrations, respectively which were also observed in optimized LORA-NLCs-2 spectra. This suggests no possible interaction between LORA and excipients and confirms the stability of prepared LORA-NLCs (Emami et al, 2020 ).…”

Section: Resultssupporting

confidence: 75%

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

et al. 2022

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Loratadine (LORA), is a topical antihistamine utilized in the treatment of ocular symptoms of COVID-19. The study aimed to develop a Loratadine Nanostructured Lipid Carriers Ocugel (LORA-NLCs Ocugel), enhance its solubility, trans-corneal penetrability, and bioavailability. full-factorial design was established with 2 4 trials to investigate the impact of several variables upon NLCs properties. LORA-NLCs were fabricated by using hot melt emulsification combined with high-speed stirring and ultrasonication methods. All obtained formulae were assessed in terms of percent of entrapment efficiency (EE%), size of the particle (PS), zeta potential (ZP), as well as in-vitro release. Via using Design Expert® software the optimum formula was selected, characterized using FTIR, Raman spectroscopy, and stability studies. Gel-based of optimized LORA-NLCs was prepared using 4% HPMC k100m which was further evaluated in terms of physicochemical properties, Ex-vivo, and In-vivo studies. The optimized LORA-NLCs, comprising Compritol 888 ATO ® , Labrasol ® , and Span ® 60 showed EE% of 95.78 ± 0.67%, PS of 156.11 ± 0.54 nm, ZP of −40.10 ± 0.55 Mv, and Qh6% of 99.67 ± 1.09%, respectively. Additionally, it illustrated a spherical morphology and compatibility of LORA with other excipients. Consequently, gel-based on optimized LORA-NLCs showed pH (7.11 ± 0.52), drug content (98.62%± 1.31%), viscosity 2736 cp, and Q12% (90.49 ± 1.32%). LORA-NLCs and LORA-NLCs Ocugel exhibited higher ex-vivo trans-corneal penetrability compared with the aqueous drug dispersion. Confocal laser scanning showed valuable penetration of fluoro-labeled optimized formula and LORA-NLCs Ocugel through corneal. The optimized formula was subjected to an ocular irritation test (Draize Test) that showed the absence of any signs of inflammation in rabbits, and histological analysis showed no effect or damage to rabbit eyeballs. C max and the AUC 0–24 were higher in LORA-NLCs Ocugel compared with pure Lora dispersion-loaded gel The research findings confirmed that NLCs could enhance solubility, trans-corneal penetrability, and the bioavailability of LORA.

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Section: Resultssupporting

confidence: 75%

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

et al. 2022

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“…The XRPD diffractogram of raw loratadine showed its crystalline nature through numerous sharp peaks between 3 and 33 degrees of the 2-θ scale, at 12.7, 15.1, 16.5, 19.7, 21.3, 23.9, 30.5, and 32.5 degrees [ 42 ]. The overlapped patterns highlight the characteristic peaks of loratadine in the OL formulations.…”

Section: Resultsmentioning

confidence: 99%

“…The increase in loratadine content that resulted in lower fractions of milk in the samples led to less intense signals of the milk constituents. All the characteristic peaks of loratadine were identified when included in the freeze-dried milk matrix, including the carbonyl band, but shifted to a lower wavenumber due to newly formed intermolecular hydrogen bonds [ 42 ]. As the FTIR results indicate the formation of new hydrogen bonding and no covalent bonds, the API shows good compatibility with the milk matrix [ 43 ].…”

Section: Resultsmentioning

confidence: 99%

Milk Oral Lyophilizates with Loratadine: Screening for New Excipients for Pediatric Use

et al. 2022

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The development of suitable formulations for the pediatric population remains a challenging field with great advances reported every year in terms of excipients and technology. When developing pediatric formulations, the acceptability of medicines represents a key element to consider. For this reason, milk can be a widely accepted excipient with taste-masking properties and supplementary advantages for drug solubility. In recent years, the orodispersible dosage forms have come onto the market as child-friendly formulations. The current study aimed to develop freeze-dried orodispersible dosage forms containing bovine milk or infant formulae as the main component. In the first stage, an exploratory study evaluated the mechanical properties of placebo milk formulations and the suitability of milk as a matrix-forming agent. As the appropriate mechanical strength to withstand manipulation was demonstrated, milk oral lyophilizates were loaded with a poorly soluble model API, loratadine. Hence, a D-optimal design was conducted to prepare milk lyophilizates with loratadine and to evaluate the effects of three factors (dose of loratadine, the lyophilizate size, and the type of milk) and their interactions. Finally, three formulations were prepared to confront the predictions of the DoE and further studied to thoroughly understand the observed effects. The experimental results showed the potential of milk in the development of oral lyophilizates loaded with different doses of suspended API.

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“…Spray-drying (chitosan-graphene oxide) [14] Freeze-drying (Sulfasalazine-chitosan) [15] Vacuum-drying (Itraconazole) [16] Aerosol flow reactor (glucocorticosteroid) [17] Electrospraying (Medroxyprogesterone acetate -PLA) [18] Fluid-bed coating/granulation/drying (Indomethacin) [19] Wet-casing drying (Sunitinib-PHBV) [20] Nanoextrusion (Griseofulvin) [21] Precipitation methods Solvent-antisolvent (Glibenclamide-HPMC) [22] High-gravity precipitation (Sorafenib) [23] Flash precipitation (soybean protein) [24] Sonocrystallization (Nobiletin) [25] Confined impinging liquid jet precipitation (loratadine) [26] Multi-inlet vortex mixing (lysozyme and erythromycin) [27] Sono precipitation (Clotrimazole, Isradipine) [28,29] Supercritical fluid precipitation (Rosuvastatin calcium) [30] Top-down High-pressure homogenization Microfluidification (Gadolinium diethylenetriamine penta-acetic acid) [31] Piston gap homogenization Bead milling (Griseofulvin -hydroxypropyl cellulose and sodium dodecyl sulfate) [32] Cryomilling (Phenytoin-PVP) [33] magnitude proportional to the concentration gradient and characterizing solute behavior, and Fick's second law, which predicts the effect of diffusion on varying concentrations. One can classify solute diffusion as either Fickian or non-Fickian, into one of which drug delivery systems frequently fall.…”

Section: Bottom-up Evaporation Methodsmentioning

confidence: 99%

Kinetic Modeling to Explain the Release of Medicine from Drug Delivery Systems

Askarizadeh,

Esfandiari,

Honarvar

et al. 2023

ChemBioEng Reviews

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Proper medication dissolution must be ensured when developing or manufacturing a new solid dosage form. Quantitative analyses performed in dissolution or release tests become simpler when applying mathematical formulae which represent dissolution outcomes as a function of several dosage form properties. Methodologies utilized to examine the kinetics of drug release from controlled‐release formulations are reviewed. The analysis of variance was conducted using statistical, model‐independent, and ‐dependent techniques for the dissolution profile comparison and fitting, respectively. Model equations, including zero‐ and first‐order, Hixson‐Crowell, Weibull, Higuchi, Korsmeyer‐Peppas, Baker‐Lonsdale, Hopfenberg, etc., were employed to match the experimental data. Additional release parameters were taken to illustrate the drug release patterns. Using correlation factors and the Akaike information criterion (AIC), the best‐fitting model was discovered, as were the transport phenomena affecting the behavior of the recognized formulations.

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Experimental study on the reduction of loratadine particle size through confined liquid impinging jets

Cited by 8 publications

References 36 publications

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

Milk Oral Lyophilizates with Loratadine: Screening for New Excipients for Pediatric Use

Kinetic Modeling to Explain the Release of Medicine from Drug Delivery Systems

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