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Pharmaceutics
Special Issues
Formulation of Photosensitive Drugs
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Formulation of Photosensitive Drugs

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (31 January 2023) | Viewed by 32162

Special Issue Editors

Dr. Giuseppina Ioele

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Guest Editor
Department of Pharmacy, Health and Nutritional Science, University of Calabria, 87036 Rende, CS, Italy
Interests: drug stability; photodegradation; light-stable formulations
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Gaetano Ragno

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Guest Editor
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Rende (CS), Italy
Interests: drug analysis; drug photostability; chemometrics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The photostability studies of a drug have assumed great importance in recent decades. The most frequent effect in the drug photodegradation is the loss of its pharmacological activity, but, in several cases, the process can involve the formation of toxic products.

The monitoring system is nowadays regulated by the international guidelines from ICH (International Conference on Harmonization), which arranges the photostability study of both the drug and its pharmaceutical forms.

Several methods for the monitoring of photosensitive drugs have been proposed, largely based on spectrophotometric, chromatographic, and multivariate analytical data processing.

Alongside the traditional methods of protecting the drug from light by means of opaque containers, there is great interest in alternative approaches based on photoprotective matrices. The most studied matrices are those enriched with photoabsorbent excipients or the polymeric and supramolecular matrices. The latter, in particular, combine the photoprotective effect with the ability to vehicular drugs with different physical–chemical features.

Dr. Giuseppina Ioele
Prof. Dr. Gaetano Ragno
Guest Editors

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Keywords

  • drug stability
  • photosensitive drugs
  • photodegradation
  • photoprotective systems
  • UV-absorbers
  • polymeric light-stable formulations
  • supramolecular light-stable formulations

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Published Papers (7 papers)

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Research

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12 pages, 1703 KiB  
Article
Structure Determination of Felodipine Photoproducts in UV-Irradiated Medicines Using ESI-LC/MS/MS
by Kohei Kawabata, Miya Kohashi, Shiori Akimoto and Hiroyuki Nishi
Pharmaceutics 2023, 15(2), 697; https://doi.org/10.3390/pharmaceutics15020697 - 19 Feb 2023
Cited by 5 | Viewed by 2089
Abstract
Dihydropyridine drugs are well known as photodegradable pharmaceuticals. Herein, we evaluate the photostability of felodipine (FL) medicine (Splendil® (SPL) tablets) and its altered forms (powders and suspensions). FL is a type of dihydropyridine drug, but its photochemical behavior is unknown. FL contents [...] Read more.
Dihydropyridine drugs are well known as photodegradable pharmaceuticals. Herein, we evaluate the photostability of felodipine (FL) medicine (Splendil® (SPL) tablets) and its altered forms (powders and suspensions). FL is a type of dihydropyridine drug, but its photochemical behavior is unknown. FL contents after ultraviolet light (UV) irradiation for 24 h were monitored using high-performance liquid chromatography (HPLC). Values of the residual amounts of FL in UV-irradiated SPL powders and suspensions were 32.76 ± 4.88% and 0.79 ± 0.74%, respectively, with the generation of two photoproducts (FL photoproduct 1 and 2). To identify the chemical structures of these photoproducts, electrospray ionization liquid chromatography mass spectrometry (ESI-LC/MS/MS) analysis was performed. Based on their mass-to-charge ratio values and fragment patterns, it was proposed that FL photoproduct 1 was a pyridine derivative and FL photoproduct 2 was an FL dimer. Interestingly, generation rates of FL photoproduct 1 and 2 were dependent on the presence of the aqueous media. The photodimerization of FL was induced in UV-irradiated SPL suspensions. This is the first report evaluating the photostability of SPL tablets and its altered forms and estimating FL photoproducts induced by UV irradiation in the formulation of SPL. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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23 pages, 10356 KiB  
Article
Photodegradation of the H1 Antihistaminic Topical Drugs Emedastine, Epinastine, and Ketotifen and ROS Tests for Estimations of Their Potent Phototoxicity
by Anna Gumieniczek, Anna Berecka-Rycerz, Urszula Hubicka, Paweł Żmudzki, Karolina Lejwoda and Paweł Kozyra
Pharmaceutics 2020, 12(6), 560; https://doi.org/10.3390/pharmaceutics12060560 - 17 Jun 2020
Cited by 6 | Viewed by 3058
Abstract
In this study, important H1 antihistaminic drugs, i.e., emedastine (EME), epinastine (EPI), and ketotifen (KET), were irradiated with UV/Vis light (300–800 nm) in solutions of different pH values. Next, they were analyzed by new high performance liquid chromatography (HPLC) methods, in order [...] Read more.
In this study, important H1 antihistaminic drugs, i.e., emedastine (EME), epinastine (EPI), and ketotifen (KET), were irradiated with UV/Vis light (300–800 nm) in solutions of different pH values. Next, they were analyzed by new high performance liquid chromatography (HPLC) methods, in order to estimate the percentage of degradation and respective kinetics. Subsequently, ultra-performance liquid chromatography tandem-mass spectrometry (UPLC-MS/MS) was used to identify their photodegradation products and to propose degradation pathways. In addition, the peroxidation of linoleic acid and generation of singlet oxygen (SO) and superoxide anion (SA) were examined, together with the molar extinction coefficient (MEC) evaluation, to estimate their phototoxic risk. The photodegradation of all EME, EPI, and KET followed pseudo first-order kinetics. At pH values of 7.0 and 10.0, EPI was shown to be rather stable. However, its photostability was lower at pH 3.0. EME was shown to be photolabile in the whole range of pH values. In turn, KET was shown to be moderately labile at pH 3.0 and 7.0. However, it degraded completely in the buffer of pH 10.0. As a result, several photodegradation products were separated and identified using the UPLC-MS/MS method. Finally, our ROS assays showed a potent phototoxic risk in the following drug order: EPI < EME < KET. All of these results may be helpful for manufacturing, storing, and applying these substantial drugs, especially in their ocular formulations. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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14 pages, 2646 KiB  
Article
Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System
by Fedora Grande, Gaetano Ragno, Rita Muzzalupo, Maria Antonietta Occhiuzzi, Elisabetta Mazzotta, Michele De Luca, Antonio Garofalo and Giuseppina Ioele
Pharmaceutics 2020, 12(5), 423; https://doi.org/10.3390/pharmaceutics12050423 - 5 May 2020
Cited by 14 | Viewed by 3411
Abstract
Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, were applied on ethanol solutions and topical [...] Read more.
Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, were applied on ethanol solutions and topical gel formulations of both compounds. The photodegradation profiles were monitored by Multivariate curve resolution applied to the UV spectral data. The inclusion of the compounds in microemulsion was investigated to improve light stability and, at the same time, to ensure a sustained release system for skin delivery. All the formulations in solution, gel, microemulsion, and microemulsion-in-gel were exposed to a forced irradiation of 350 W/m2, corresponding to a 21 kJ/m2 min, for up to 300 min. Photostability increased significantly for both drugs in the liquid microemulsion and microemulsion-in-gel, compared to the ethanol solution and plain gel, reaching a residual drug of 97% and 98% for Nabumetone and analog in microemulsion-in-gel, respectively. Permeation experiments on the microemulsion-in-gel showed a better performance of the analog formulated at 0.2%, compared to the same formulation of Nabumetone at 0.7%. These results highlight the potential of the designed matrices as delayed drug delivery systems along with the use of lower drug doses leading to reduced side effects. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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26 pages, 4754 KiB  
Article
π-π-Stacked Poly(ε-caprolactone)-b-poly(ethylene glycol) Micelles Loaded with a Photosensitizer for Photodynamic Therapy
by Yanna Liu, Marcel H.A.M. Fens, Bo Lou, Nicky C.H. van Kronenburg, Roel F.M. Maas-Bakker, Robbert J. Kok, Sabrina Oliveira, Wim E. Hennink and Cornelus F. van Nostrum
Pharmaceutics 2020, 12(4), 338; https://doi.org/10.3390/pharmaceutics12040338 - 9 Apr 2020
Cited by 10 | Viewed by 3271
Abstract
To improve the in vivo stability of poly(ε-caprolactone)-b-poly(ethylene glycol) (PCL-PEG)-based micelles and cargo retention by π-π stacking interactions, pendant aromatic rings were introduced by copolymerization of ε-caprolactone with benzyl 5-methyl-2-oxo-1,3-dioxane-5-carboxylate (TMC-Bz). It was shown that the incorporation of aromatic rings yielded [...] Read more.
To improve the in vivo stability of poly(ε-caprolactone)-b-poly(ethylene glycol) (PCL-PEG)-based micelles and cargo retention by π-π stacking interactions, pendant aromatic rings were introduced by copolymerization of ε-caprolactone with benzyl 5-methyl-2-oxo-1,3-dioxane-5-carboxylate (TMC-Bz). It was shown that the incorporation of aromatic rings yielded smaller micelles (18–30 nm) with better colloidal stability in PBS than micelles without aromatic groups. The circulation time of i.v. injected micelles containing multiple pendant aromatic groups was longer (t½-α: ~0.7 h; t½-β: 2.9 h) than that of micelles with a single terminal aromatic group (t½ < 0.3 h). In addition, the in vitro partitioning of the encapsulated photosensitizer (meta-tetra(hydroxyphenyl)chlorin, mTHPC) between micelles and human plasma was favored towards micelles for those that contained the pendant aromatic groups. However, this was not sufficient to fully retain mTHPC in the micelles in vivo, as indicated by similar biodistribution patterns of micellar mTHPC compared to free mTHPC, and unequal biodistribution patterns of mTHPC and the host micelles. Our study points out that more detailed in vitro methods are necessary to more reliably predict in vivo outcomes. Furthermore, additional measures beyond π-π stacking are needed to stably incorporate mTHPC in micelles in order to benefit from the use of micelles as targeted delivery systems. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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Review

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37 pages, 4260 KiB  
Review
Drug Delivery Strategies for Avobenzone: A Case Study of Photostabilization
by Amol D. Gholap, Sadikali F. Sayyad, Navnath T. Hatvate, Vilas V. Dhumal, Sagar R. Pardeshi, Vivek P. Chavda and Lalitkumar K. Vora
Pharmaceutics 2023, 15(3), 1008; https://doi.org/10.3390/pharmaceutics15031008 - 21 Mar 2023
Cited by 23 | Viewed by 6577
Abstract
Several developments and research methods are ongoing in drug technology and chemistry research to elicit effectiveness regarding the therapeutic activity of drugs along with photoprotection for their molecular integrity. The detrimental effect of UV light induces damaged cells and DNA, which leads to [...] Read more.
Several developments and research methods are ongoing in drug technology and chemistry research to elicit effectiveness regarding the therapeutic activity of drugs along with photoprotection for their molecular integrity. The detrimental effect of UV light induces damaged cells and DNA, which leads to skin cancer and other phototoxic effects. The application of sunscreen shields to the skin is important, along with recommended UV filters. Avobenzone is widely used as a UVA filter for skin photoprotection in sunscreen formulations. However, keto-enol tautomerism propagates photodegradation into it, which further channelizes the phototoxic and photoirradiation effects, further limiting its use. Several approaches have been used to counter these issues, including encapsulation, antioxidants, photostabilizers, and quenchers. To seek the gold standard approach for photoprotection in photosensitive drugs, combinations of strategies have been implemented to identify effective and safe sunscreen agents. The stringent regulatory guidelines for sunscreen formulations, along with the availability of limited FDA-approved UV filters, have led many researchers to develop perfect photostabilization strategies for available photostable UV filters, such as avobenzone. From this perspective, the objective of the current review is to summarize the recent literature on drug delivery strategies implemented for the photostabilization of avobenzone that could be useful to frame industrially oriented potential strategies on a large scale to circumvent all possible photounstable issues of avobenzone. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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17 pages, 9692 KiB  
Review
Latest Evidence Regarding the Effects of Photosensitive Drugs on the Skin: Pathogenetic Mechanisms and Clinical Manifestations
by Flavia Lozzi, Cosimo Di Raimondo, Caterina Lanna, Laura Diluvio, Sara Mazzilli, Virginia Garofalo, Emi Dika, Elena Dellambra, Filadelfo Coniglione, Luca Bianchi and Elena Campione
Pharmaceutics 2020, 12(11), 1104; https://doi.org/10.3390/pharmaceutics12111104 - 17 Nov 2020
Cited by 20 | Viewed by 6462
Abstract
Photosensitivity induced by drugs is a widely experienced problem, concerning both molecule design and clinical practice. Indeed, photo-induced cutaneous eruptions represent one of the most common drug adverse events and are frequently an important issue to consider in the therapeutic management of patients. [...] Read more.
Photosensitivity induced by drugs is a widely experienced problem, concerning both molecule design and clinical practice. Indeed, photo-induced cutaneous eruptions represent one of the most common drug adverse events and are frequently an important issue to consider in the therapeutic management of patients. Phototoxicity and photoallergy are the two different pathogenic mechanisms involved in photosensitization. Related cutaneous manifestations are heterogeneous, depending on the culprit drug and subject susceptibility. Here we report an updated review of the literature with respect to pathogenic mechanisms of photosensitivity, clinical manifestations, patient management, and prediction and evaluation of drug-induced photosensitivity. We present and discuss principal groups of photosensitizing drugs (antimicrobials, nonsteroidal anti-inflammatory drugs, anti-hypertensives, anti-arrhythmics, cholesterol, and glycemia-lowering agents, psychotropic drugs, chemotherapeutics, etc.) and their main damage mechanisms according to recent evidence. The link between the drug and the cutaneous manifestation is not always clear; more investigations would be helpful to better predict drug photosensitizing potential, prevent and manage cutaneous adverse events and find the most appropriate alternative therapeutic strategy. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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33 pages, 2061 KiB  
Review
Recent Advances in the Structural Design of Photosensitive Agent Formulations Using “Soft” Colloidal Nanocarriers
by Agata Pucek, Beata Tokarek, Ewelina Waglewska and Urszula Bazylińska
Pharmaceutics 2020, 12(6), 587; https://doi.org/10.3390/pharmaceutics12060587 - 24 Jun 2020
Cited by 46 | Viewed by 5960
Abstract
The growing demand for effective delivery of photosensitive active compounds has resulted in the development of colloid chemistry and nanotechnology. Recently, many kinds of novel formulations with outstanding pharmaceutical potential have been investigated with an expansion in the design of a wide variety [...] Read more.
The growing demand for effective delivery of photosensitive active compounds has resulted in the development of colloid chemistry and nanotechnology. Recently, many kinds of novel formulations with outstanding pharmaceutical potential have been investigated with an expansion in the design of a wide variety of “soft” nanostructures such as simple or multiple (double) nanoemulsions and lipid formulations. The latter can then be distinguished into vesicular, including liposomes and “smart” vesicles such as transferosomes, niosomes and ethosomes, and non-vesicular nanosystems with solid lipid nanoparticles and nanostructured lipid carriers. Encapsulation of photosensitive agents such as drugs, dyes, photosensitizers or antioxidants can be specifically formulated by the self-assembly of phospholipids or other amphiphilic compounds. They are intended to match unique pharmaceutic and cosmetic requirements and to improve their delivery to the target site via the most common, i.e., transdermal, intravenous or oral administration routes. Numerous surface modifications and functionalization of the nanostructures allow increasing their effectiveness and, consequently, may contribute to the treatment of many diseases, primarily cancer. An increasing article number is evidencing significant advances in applications of the different classes of the photosensitive agents incorporated in the ”soft” colloidal nanocarriers that deserved to be highlighted in the present review. Full article
(This article belongs to the Special Issue Formulation of Photosensitive Drugs)
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