Preparation of Ascorbic Acid and Cholecalciferol Microsponges for Topical Application

Zia, Rabia; Nazir, Akmal; Khan, Muhammad Kashif Iqbal; Maan, Abid Aslam; Rashid, Ayesha

doi:10.22159/ijpps.2017v9i10.17525

Cited by 4 publications

(3 citation statements)

References 24 publications

(33 reference statements)

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“…Since the middle of the last century, the stability of ascorbic acid (AA), which has antioxidant properties in mammals and in foodstuffs, has been actively studied [1][2][3][4][5][6][7][8][9]. AA degradation can occur spontaneously, even in an anaerobic environment, and under the influence of a number of factors [1,2,5].…”

Section: Introductionmentioning

confidence: 99%

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

Сыроешкин¹,

Pleteneva²,

Uspenskaya³

et al. 2019

Int J App Pharm

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Objective: To investigate the thermal stability of aqueous solutions of L-ascorbic acid (AA) and its reactions with excipients for the improvement of the injection forms technology. Methods: Solutions of L-ascorbic acid were prepared using deuterium depleted water (DDW-«light» water, D/H=4 ppm) and natural deionized high-ohmic water (BD, D/H=140 ppm). The optical rotation was observed using an automatic polarimeter Atago POL-1/2. Electrospray tandem mass spectra were recorded by Sciex X500R QTOF. Electronic spectra were recorded by UV-spectrometer Cary 60 (Agilent). Unicellular biosensor (Spirotox-test) was used for investigation of excipients influence on the AA biological activity. The statistical analysis was carried out using the OriginPro®9 packages. Results: The results demonstrate the thermal instability of AA. The optical activity of injection forms of AA differs from model solutions with the same concentration and pH value but without heat treatment. Monitoring of solutions by the LC-ESI-MS/MS method made it possible to characterize the nature of some thermal decomposition products. Thermodynamic calculations and evaluation of biological activity (Spirotox-test) indicate that AA interacts with sulfite-ion by redox mechanisms. Excipients in AA aqueous solutions decrease, but DDW increases the biological object lifetime. Conclusion: The use of the set of physicochemical and biological methods to study the effect of heat treatment of L-ascorbic acid solutions in the presence of sulfur (IV) compounds as excipients made it possible to identify decomposition products of the active pharmaceutical ingredient. The results indicate the need to exclude sterilization of the AA injection form by the thermal method and replace it with an alternative one, for example, with gamma radiation treatment.

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Section: Introductionmentioning

confidence: 99%

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

Сыроешкин¹,

Pleteneva²,

Uspenskaya³

et al. 2019

Int J App Pharm

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“…Two other characteristic peaks are found around the values of 1744 and 1112 cm −1 , representing the stretching vibrations of C=O and C-O-C bonds, respectively. Since BG was deposited as a thin film together with VD3, the presence of Si-O-Si groups can also be observed [40,42]. However, from the point of view of the efficient transfer of the composite material and the preservation of chemical integrity, optimal results were revealed for the BG+VD3_025 samples.…”

Section: Surface Investigation Of As-deposited Thin Filmsmentioning

confidence: 99%

Bioglass and Vitamin D3 Coatings for Titanium Implants: Osseointegration and Corrosion Protection

Negut,

Gradisteanu-Pircalabioru,

Dinu

et al. 2023

Biomedicines

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The use of MAPLE synthesized thin films based on BG and VD3 for improving the osseointegration and corrosion protection of Ti-like implant surfaces is reported. The distribution of chemical elements and functional groups was shown by FTIR spectrometry; the stoichiometry and chemical functional integrity of thin films after MAPLE deposition was preserved, optimal results being revealed especially for the BG+VD3_025 samples. The morphology and topography were examined by SEM and AFM, and revealed surfaces with many irregularities, favoring a good adhesion of cells. The thin films’ cytotoxicity and biocompatibility were evaluated in vitro at the morphological, biochemical, and molecular level. Following incubation with HDF cells, BG57+VD3_ 025 thin films showed the best degree of biocompatibility, as illustrated by the viability assay values. According to the LDH investigation, all tested samples had higher values compared to the unstimulated cells. The evaluation of cell morphology was performed by fluorescence microscopy following cultivation of HDF cells on the obtained thin films. The cultivation of HDF’s on the thin films did not induce major cellular changes. Cells cultured on the BG57+VD3_025 sample had similar morphology to that of unstimulated control cells. The inflammatory profile of human cells cultured on thin films obtained by MAPLE was analyzed by the ELISA technique. It was observed that the thin films did not change the pro- and anti-inflammatory profile of the HDF cells, the IL-6 and IL-10 levels being similar to those of the control sample. The wettability of the MAPLE thin films was investigated by the sessile drop method. A contact angle of 54.65° was measured for the sample coated with BG57+VD3_025. Electrochemical impedance spectroscopy gave a valuable insight into the electrochemical reactions occurring on the surface.

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“…Filtered sample was suitably diluted with 0.75% w/v PVA solution and analyzed spectrophotometrically at 354 nm using ultraviolet (UV)-Vis spectrophotometer. Percentage of the unentrapped drug was calculated [13].…”

Section: Yieldmentioning

confidence: 99%

Formulation and Evaluation of Lornoxicam Microsponges Using Eudragit Rs 100 and Eudragit Rspo

Thireesha¹,

Prasad²,

L³

2018

Asian J Pharm Clin Res

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Objective: The objective of the present study was preparation and evaluation of lornoxicam microsponges to prolong their drug release up to 12 h for effective osteoarthritis, rheumatoid arthritis, and acute lumbar-sciatica therapy.Methods: Lornoxicam microsponges were prepared by the quasi-emulsion solvent diffusion technique using different concentrations of polymers such as Eudragit RS 100 and Eudragit RSPO in ethanol and dichloromethane organic solvent mixture. Microsponges were evaluated for their particle size, percentage yield, entrapment efficiency, scanning electron microscopy (SEM), and in vitro drug release studies.Results: The percentage yield, entrapment efficiency, average particle size, and in vitro drug release for optimized formulation F12 were found to be 70.23% w/w, 81.34% w/w, 172.72 μm, and 96.64% up to 8 h, respectively. From SEM, it was observed that microsponges were found to be spherical in shape with rough surface texture. The formulation F12 shows zero-order release kinetics with an r2 value of 0.961 and the value of Korsmeyer–Peppas model was found to be 0.792; it follows super case II non-Fickian diffusion. The in vitro drug release studies showed that formulations comprised varying concentrations of Eudragit RSPO in higher proportion exhibited much-retarded drug release as compared to formulations comprised a higher proportion of varying concentrations of Eudragit RS 100.Conclusion: Among all the formulations F12 shows better results, which are released more than 80% of the drug release within 8 h; hence, it is optimized. These developed microsponges are releasing the drug for a longer period, which will be effective for osteoarthritis, rheumatoid arthritis, and acute lumbar sciatica therapy.

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Preparation of Ascorbic Acid and Cholecalciferol Microsponges for Topical Application

Cited by 4 publications

References 24 publications

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

Bioglass and Vitamin D3 Coatings for Titanium Implants: Osseointegration and Corrosion Protection

Formulation and Evaluation of Lornoxicam Microsponges Using Eudragit Rs 100 and Eudragit Rspo

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