Formulation and stabilization of riboflavin in liposomal preparations

Ahmad, Iqbal; Arsalan, Adeel; Ali, Syed Abid; Sheraz, Muhammad Ali; Ahmed, Sofia; Anwar, Zubair; Munir, Iqra; Shah, Muhammad Raza

doi:10.1016/j.jphotobiol.2015.10.017

Cited by 25 publications

(40 citation statements)

References 65 publications

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“…The method has been validated prior to its application to the assay of B 12 in liposomal preparations (Table ). Since B 12 is present in liposomal preparations and the lipid particles interfere in the spectrometric assay of B 12 and B 12b as observed earlier in the case of the assay of riboflavin in liposomes, a modification of the method has been applied. The absorption spectra of photolyzed solution of B 12 are shown in Figure 3A, which clearly indicate the presence of an isosbestic point around 535 nm, indicating the transformation of B 12 to B 12b on visible irradiation.…”

Section: Resultsmentioning

confidence: 99%

“…In the light of previous studies, the interaction of PC and B12 may be described by a scheme involving the reactions given below:

[{normalB}_{12}] \overset{h v}{\to}^{1} false[B_{12} false]

^{1} [{normalB}_{12} false] + normalPC \overset{}{\to} {B_{12}}^{• -} + P {normalC}^{• +}

\underset{(charge - transfer complex)}{{false[}^{1} {normalB}_{12} \dots PC false] ⟷ [^{1} {normalB}_{12}^{• -} \dots normalP C^{• +} false] \to {B_{12}}^{• -} + P {normalC}^{• +}}

{B_{12}}^{• -} \overset{- e^{-}}{\to} {normalB}_{12}

P {normalC}^{• +} \overset{+ e^{-}}{\to} PC

…”

Section: Resultsmentioning

confidence: 99%

“…Liposomes were prepared as described by Ahmad et al . The preparation of liposomes was based on a variation in PC content (10.80‐16.20 mM) at a constant concentration of CH (13.50 mM) (Table ).…”

Section: Methodsmentioning

confidence: 99%

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The kinetics of photostabilization of cyanocobalamin in liposomal preparations

Arsalan

Ahmad

Ali

et al. 2020

Int J of Chemical Kinetics

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Cyanocobalamin (B 12 ) is a photosensitive vitamin, and its photodegradation to hydroxocobalamin (B 12b ) in liposomes has been investigated. The values of apparent first-order rate constants (k obs ) for the photodegradation of B 12 in liposomes (nine preparations) are in the range of (0.52-2.24) × 10 -3 min -1 , compared to 3.21 × 10 -3 min -1 for B 12 in aqueous solution (pH 5.0). The entrapment efficiency of B 12 in liposomes is 26.4-38.8%. The values of k obs show a linear relation with phosphatidylcholine (PC) content in liposomes, indicating the influence of PC in inhibiting the rate of photolysis of B 12 . The value of the bimolecular rate constant for photochemical interaction of B 12 and PC is 0.32 M -1 min -1 , indicating the stabilizing effect of PC on the photolysis of B 12 . The ratio of B 12 stabilization in liposomal preparations is in the range 2-6 compared to that of the unentrapped vitamin The stabilization of B 12 is mediated by a photoinduced charge-transfer B 12 -PC complex that leads to the reduction of B 12 to B 12r , which is then oxidized to B 12b that has low susceptibility to photolysis. The extent of stabilization of B 12 probably depends on the degree of interaction between the two compounds under the reaction conditions, indicated by the loss of B 12 fluorescence.

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Section: Resultsmentioning

confidence: 99%

“…In the light of previous studies, the interaction of PC and B12 may be described by a scheme involving the reactions given below:

[{normalB}_{12}] \overset{h v}{\to}^{1} false[B_{12} false]

^{1} [{normalB}_{12} false] + normalPC \overset{}{\to} {B_{12}}^{• -} + P {normalC}^{• +}

\underset{(charge - transfer complex)}{{false[}^{1} {normalB}_{12} \dots PC false] ⟷ [^{1} {normalB}_{12}^{• -} \dots normalP C^{• +} false] \to {B_{12}}^{• -} + P {normalC}^{• +}}

{B_{12}}^{• -} \overset{- e^{-}}{\to} {normalB}_{12}

P {normalC}^{• +} \overset{+ e^{-}}{\to} PC

…”

Section: Resultsmentioning

confidence: 99%

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The kinetics of photostabilization of cyanocobalamin in liposomal preparations

Arsalan

Ahmad

Ali

et al. 2020

Int J of Chemical Kinetics

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“…Photostabilization of the drug substances by entrapment into liposomes is an effective method to improve their photostability. Examples of stabilization of the photosensitive drugs in liposomal formulations include riboflavin [163][164][165][166][167], doxorubicin [168], vitamin A palmitate [169], fluoroquinolones [170,171], rose Bengal [172], amlodipine [173], tretinoin [174], 2,7-dichlorodihydrofluorescein [175], opalmitoyl amylopectin [176], and zinc phthalocyanine and chloroaluminium phthalocyanine [177]. The entrapment efficiency of the liposomes facilitates the enhancement of the photostability of the drugs [164,165,174,178].…”

Section: Liposome Formationmentioning

confidence: 99%

Photostability and Photostabilization of Drugs and Drug Products

Ahmad

Ahmed

Anwar

et al. 2016

International Journal of Photoenergy

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120

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Photostability studies of drugs and drug products are an integral part of the product development process in the pharmaceutical industry. These studies are carried out to ensure quality, efficacy, and safety of the formulated products during manufacture, storage, and use. This review deals with the concept of photostability and related aspects and the literature available in the field. It highlights the role of the photochemistry in the photostability studies, describes the functional groups important for the photoreactivity of drugs, explains photophysical processes, and deals with the kinetics of photochemical reactions. The various modes of photodegradation of drugs with examples of selected compounds are presented. The biological consequences of the effect of light on the drug degradation are described. The photostability testing of drugs and drug products and the requirements under ICH guideline are discussed. Some information on the packaging requirements for the formulated products is provided. The various methods used for the photostabilization of solid and liquid dosage forms are also discussed.

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“…Liposomal formulations of riboflavin were previously studied in tumor targeting and were reported to achieve improvements in riboflavin's photostabilization [33,34]. However, to the best of our knowledge, there is no report in the literature on how incorporation of RbP into liposomal carriers will affect the transcorneal permeation of this drug.…”

Section: Preparation and Characterisation Of Liposomes With Rbpmentioning

confidence: 99%

Delivery of Riboflavin-5′-Monophosphate Into the Cornea: Can Liposomes Provide Any Enhancement Effects?

Kandžija

Khutoryanskiy

2017

Journal of Pharmaceutical Sciences

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Keratoconus is a progressive condition caused by the thinning of the cornea, which eventually deforms the front surface of the eye into a cone shape leading to ghosting, multiple images, glare, and several other vision problems. Currently, keratoconus is treated with UV-induced riboflavin (Rb)-mediated collagen cross-linking, which requires a physical removal of the corneal epithelium under topical anesthesia. This study reports the penetration of Rb and its more water-soluble form, riboflavin-5'-monophosphate (RbP), into the bovine cornea ex vivo. Using ex vivo bovine corneal tissues and 0.8 mg/mL drug solutions in phosphate buffer, it was established that RbP penetration into the cornea within 3 h of diffusion experiment was greater (17.3 ± 0.8 μg) compared with Rb (10.4 ± 4.2 μg). In the cornea, RbP was found to convert to Rb, which is mediated with enzymes present in this tissue. Several formulations including the conventional and propylene glycol-containing liposomes with encapsulated RbP have been developed, and their effect on the drug penetration into the bovine cornea was evaluated. Encapsulation of RbP into the liposomes did not provide any statistically significant improvement in the penetration of RbP into the cornea.

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Formulation and stabilization of riboflavin in liposomal preparations

Cited by 25 publications

References 65 publications

The kinetics of photostabilization of cyanocobalamin in liposomal preparations

The kinetics of photostabilization of cyanocobalamin in liposomal preparations

Photostability and Photostabilization of Drugs and Drug Products

Delivery of Riboflavin-5′-Monophosphate Into the Cornea: Can Liposomes Provide Any Enhancement Effects?

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