Research

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15 pages, 884 KiB

Open AccessArticle

An Analytical Target Profile for the Development of an In Vitro Release Test Method and Apparatus Selection in the Case of Semisolid Topical Formulations

by Réka Szoleczky, Anita Kovács, Szilvia Berkó and Mária Budai-Szűcs

Pharmaceutics 2024, 16(3), 313; https://doi.org/10.3390/pharmaceutics16030313 - 23 Feb 2024

Viewed by 637

Abstract

This study focuses on how to define an Analytical Target Profile (ATP) which is intended for use in practice and on facilitating the selection of in vitro release test (IVRT) technology for diclofenac sodium topical hydrogel and cream. The implementation involves incorporating the [...] Read more.

This study focuses on how to define an Analytical Target Profile (ATP) which is intended for use in practice and on facilitating the selection of in vitro release test (IVRT) technology for diclofenac sodium topical hydrogel and cream. The implementation involves incorporating the new draft guidelines of the International Council for Harmonisation (ICH Q14) and USP (United States Pharmacopeia) Chapter 1220. Four IVRT apparatuses were compared (USP Apparatus II with immersion cell, USP Apparatus IV with semisolid adapter, static vertical diffusion cell, and a new, in-house-developed flow-through diffusion cell) with the help of the ATP. Performance characteristics such as accuracy, precision, cumulative amount released at the end of the IVRT experiment, and robustness were investigated. We found that the best apparatus for developing IVRT quality control (QC) tests in both cases was USP II with an immersion cell. All four different IVRT apparatuses were compared with each other and with the data found in the literature. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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17 pages, 3194 KiB

Open AccessArticle

Photodynamic Antibacterial Therapy of Gallic Acid-Derived Carbon-Based Nanoparticles (GACNPs): Synthesis, Characterization, and Hydrogel Formulation

by Koranat Dechsri, Cheewita Suwanchawalit, Prasopchai Patrojanasophon, Praneet Opanasopit, Supusson Pengnam, Thapakorn Charoenying and Theerada Taesotikul

Pharmaceutics 2024, 16(2), 254; https://doi.org/10.3390/pharmaceutics16020254 - 09 Feb 2024

Viewed by 928

Abstract

Carbon-based nanoparticles (CNPs) have gained recognition because of their good biocompatibility, easy preparation, and excellent phototherapy properties. In biomedicine applications, CNPs are widely applied as photodynamic agents for antibacterial purposes. Photodynamic therapy has been considered a candidate for antibacterial agents because of its [...] Read more.

Carbon-based nanoparticles (CNPs) have gained recognition because of their good biocompatibility, easy preparation, and excellent phototherapy properties. In biomedicine applications, CNPs are widely applied as photodynamic agents for antibacterial purposes. Photodynamic therapy has been considered a candidate for antibacterial agents because of its noninvasiveness and minimal side effects, especially in the improvement in antibacterial activity against multidrug-resistant bacteria, compared with conventional antibiotic medicines. Here, we developed CNPs from an active polyhydroxy phenolic compound, namely, gallic acid, which has abundant hydroxyl groups that can yield photodynamic effects. Gallic acid CNPs (GACNPs) were rapidly fabricated via a microwave-assisted technique at 200 °C for 20 min. GACNPs revealed notable antibacterial properties against Gram-positive and Gram-negative bacteria, including Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). The minimum inhibitory concentrations of GACNPs in S. aureus and E. coli were equal at approximately 0.29 mg/mL and considerably lower than those in gallic acid solution. Furthermore, the GACNP-loaded hydrogel patches demonstrated an attractive photodynamic effect against S. aureus, and it was superior to that of Ag hydrofiber^®, a commercial material. Therefore, the photodynamic properties of GACNPs can be potentially used in the development of antibacterial hydrogels for wound healing applications. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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18 pages, 2812 KiB

Open AccessArticle

Rheological and Viscoelastic Analysis of Hybrid Formulations for Topical Application

by Maria Natalia Calienni, Luis Manuel Martínez, Maria Cecilia Izquierdo, Silvia del Valle Alonso and Jorge Montanari

Pharmaceutics 2023, 15(10), 2392; https://doi.org/10.3390/pharmaceutics15102392 - 27 Sep 2023

Viewed by 923

Abstract

The rheological and viscoelastic properties of hybrid formulations composed of vehicles designed for cutaneous topical application and loaded with ultradeformable liposomes (UDL) were assessed. UDL were selected for their established ability to transport both lipophilic and hydrophilic compounds through the skin, and are [...] Read more.

The rheological and viscoelastic properties of hybrid formulations composed of vehicles designed for cutaneous topical application and loaded with ultradeformable liposomes (UDL) were assessed. UDL were selected for their established ability to transport both lipophilic and hydrophilic compounds through the skin, and are applicable in pharmaceuticals and cosmetics. Formulations underwent flow analysis and were fitted to the Herschel–Bulkley model due to their prevalent non-Newtonian behavior in most cases. Linear viscoelastic regions (LVR) were identified, and G′ and G″ moduli were determined via frequency sweep steps, considering the impact of temperature and aging. The formulations exhibited non-Newtonian behavior with pseudoplastic traits in most cases, with UDL incorporation inducing rheological changes. LVR and frequency sweep tests indicated predominantly elastic solid behavior, with G′ higher than G″, at different temperatures and post-production times. Tan δ values also illustrated a predominant solid-like behavior over liquid. This study provides pivotal insights into the rheological and viscoelastic features of topical formulations, emphasizing the crucial role of meticulous vehicle and formulation selection when incorporating UDL or analogous liposomal drug delivery systems. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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17 pages, 6935 KiB

Open AccessArticle

Formulation and Therapeutic Evaluation of Isoxsuprine-Loaded Nanoparticles against Diabetes-Associated Stroke

by Heba A. Abou-Taleb, Basmah Nasser Aldosari, Randa Mohammed Zaki, Obaid Afzal, Alaa S. Tulbah, Mary Girgis Shahataa, Fatma I. Abo El-Ela, Heba F. Salem and Amr Gamal Fouad

Pharmaceutics 2023, 15(9), 2242; https://doi.org/10.3390/pharmaceutics15092242 - 30 Aug 2023

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Abstract

Ischemic stroke is the second-leading cause of death. Hyperglycemia, which is characteristic of diabetes mellitus, contributes to the development of endothelial dysfunction and increases the risk of stroke. Isoxsuprine is an efficient beta-adrenergic agonist that improves blood flow to the ischemic aria and [...] Read more.

Ischemic stroke is the second-leading cause of death. Hyperglycemia, which is characteristic of diabetes mellitus, contributes to the development of endothelial dysfunction and increases the risk of stroke. Isoxsuprine is an efficient beta-adrenergic agonist that improves blood flow to the ischemic aria and stops the infarct core from growing. However, low bioavailability, a short biological half-life, and first-pass hepatic metabolism reduce the therapeutic efficacy of oral isoxsuprine. Therefore, the authors focused on developing isoxsuprine-loaded liposomes containing ethanol and propylene glycol (ILEP) formulation as nasal drops for the treatment of ischemic stroke in diabetic patients. Different ILEP formulations were optimized using Design Expert software, and the selected formulation was examined in vivo for its anti-stroke effect using a rat model of diabetes and stroke. The optimized ILEP, composed of 15% propylene glycol, 0.16% cholesterol, 10% ethanol, and 3.29% phospholipid, improved the sustainability, permeation, and targeting of isoxsuprine. Furthermore, the in vivo studies verified the improved neurological behavior and decreased dead shrunken neurons and vascular congestion of the rats treated with the optimized ILEP formulation, demonstrating its anti-stroke activity. In conclusion, our study found that treatment with an optimized ILEP formulation prevented the initiation and severity of stroke, especially in diabetic patients. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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23 pages, 3683 KiB

Open AccessArticle

In Vitro and In Vivo Efficacy of Topical Dosage Forms Containing Self-Nanoemulsifying Drug Delivery System Loaded with Curcumin

by Gréta Frei, Ádám Haimhoffer, Enikő Csapó, Krisztina Bodnár, Gábor Vasvári, Dániel Nemes, István Lekli, Alexandra Gyöngyösi, Ildikó Bácskay, Pálma Fehér and Liza Józsa

Pharmaceutics 2023, 15(8), 2054; https://doi.org/10.3390/pharmaceutics15082054 - 31 Jul 2023

Cited by 3 | Viewed by 2050

Abstract

The external use of curcumin is rare, although it can be a valuable active ingredient in the treatment of certain inflammatory diseases. The aim of our experimental work was to formulate topical dosage forms containing curcumin for the treatment of atopic dermatitis. Curcumin [...] Read more.

The external use of curcumin is rare, although it can be a valuable active ingredient in the treatment of certain inflammatory diseases. The aim of our experimental work was to formulate topical dosage forms containing curcumin for the treatment of atopic dermatitis. Curcumin has extremely poor solubility and bioavailability, so we have tried to increase it with the usage of self-emulsifying drug delivery systems. Creams and gels were formulated using penetration-enhancing surfactants and gelling agents. The release of the drug from the vehicle and its penetration through the membrane were determined using a Franz diffusion cell. An MTT cytotoxicity and in vitro antioxidant assays were performed on HaCaT cell line. The in vivo anti-inflammatory effect of the preparations was tested by measuring rat paw edema. In addition, we examined the degree of inflammation induced by UV radiation after pretreatment with the cream and the gel on rats. For the gels containing SNEDDS, the highest penetration was measured after half an hour, while for the cream, it took one hour to reach the maximum concentration. The gel containing Pemulen TR-1 showed the highest drug release. It was determined that the curcumin-containing preparations can be safely applied on the skin and have antioxidant effects. The animal experiments have proven the effectiveness of curcumin-containing topical preparations. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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Review

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26 pages, 2722 KiB

Open AccessReview

Nanomaterials in the Wound Healing Process: New Insights and Advancements

by Tanikan Sangnim, Vivek Puri, Divya Dheer, D. Nagasamy Venkatesh, Kampanart Huanbutta and Ameya Sharma

Pharmaceutics 2024, 16(3), 300; https://doi.org/10.3390/pharmaceutics16030300 - 21 Feb 2024

Cited by 1 | Viewed by 1227

Abstract

Wounds, which are becoming more common as a result of traumas, surgery, burns, and chronic illnesses like diabetes, remain a critical medical problem. Infectious bacteria impact the healing process, particularly if its biofilm (biological films) leads to a prolonged effect. Nanomaterials have emerged [...] Read more.

Wounds, which are becoming more common as a result of traumas, surgery, burns, and chronic illnesses like diabetes, remain a critical medical problem. Infectious bacteria impact the healing process, particularly if its biofilm (biological films) leads to a prolonged effect. Nanomaterials have emerged as promising candidates in the field of wound healing due to their unique properties and versatile applications. New insights into the interactions between nanomaterials and wound microenvironments have shed light on the mechanisms underlying their therapeutic effects. However, a significantly minimal amount of research has been carried out to see if these nanomaterials significantly promote the wound healing process. In this review, we provided an outline of the various types of nanomaterials that have been studied for healing wounds and infection prevention. Overall, the utilization of nanomaterials in wound healing holds great promise and continues to evolve, providing new opportunities for the development of effective and efficient wound care therapies. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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42 pages, 2857 KiB

Open AccessReview

Chemical Insights into Topical Agents in Intraocular Pressure Management: From Glaucoma Etiopathology to Therapeutic Approaches

by Geewoo Nam Patton and Hyuck Jin Lee

Pharmaceutics 2024, 16(2), 274; https://doi.org/10.3390/pharmaceutics16020274 - 15 Feb 2024

Viewed by 798

Abstract

Glaucoma encompasses a group of optic neuropathies characterized by complex and often elusive etiopathology, involvihttng neurodegeneration of the optic nerve in conjunction with abnormal intraocular pressure (IOP). Currently, there is no cure for glaucoma, and treatment strategies primarily aim to halt disease progression [...] Read more.

Glaucoma encompasses a group of optic neuropathies characterized by complex and often elusive etiopathology, involvihttng neurodegeneration of the optic nerve in conjunction with abnormal intraocular pressure (IOP). Currently, there is no cure for glaucoma, and treatment strategies primarily aim to halt disease progression by managing IOP. This review delves into the etiopathology, diagnostic methods, and treatment approaches for glaucoma, with a special focus on IOP management. We discuss a range of active pharmaceutical ingredients used in glaucoma therapy, emphasizing their chemical structure, pharmacological action, therapeutic effectiveness, and safety/tolerability profiles. Notably, most of these therapeutic agents are administered as topical formulations, a critical aspect considering patient compliance and drug delivery efficiency. The classes of glaucoma therapeutics covered in this review include prostaglandin analogs, beta blockers, alpha agonists, carbonic anhydrase inhibitors, Rho kinase inhibitors, and miotic (cholinergic) agents. This comprehensive overview highlights the importance of topical administration in glaucoma treatment, offering insights into the current state and future directions of pharmacological management in glaucoma. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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26 pages, 7027 KiB

Open AccessReview

Innovative Topical Patches for Non-Melanoma Skin Cancer: Current Challenges and Key Formulation Considerations

by Sangseo Kim, Candace M. Day, Yunmei Song, Amy Holmes and Sanjay Garg

Pharmaceutics 2023, 15(11), 2577; https://doi.org/10.3390/pharmaceutics15112577 - 03 Nov 2023

Cited by 3 | Viewed by 1339

Abstract

Non-melanoma skin cancer (NMSC) is the most prevalent malignancy worldwide, with approximately 6.3 million new cases worldwide in 2019. One of the key management strategies for NMSC is a topical treatment usually utilised for localised and early-stage disease owing to its non-invasive nature. [...] Read more.

Non-melanoma skin cancer (NMSC) is the most prevalent malignancy worldwide, with approximately 6.3 million new cases worldwide in 2019. One of the key management strategies for NMSC is a topical treatment usually utilised for localised and early-stage disease owing to its non-invasive nature. However, the efficacy of topical agents is often hindered by poor drug penetration and patient adherence. Therefore, various research groups have employed advanced drug delivery systems, including topical patches to overcome the problem of conventional topical treatments. This review begins with an overview of NMSC as well as the current landscape of topical treatments for NMSC, specifically focusing on the emerging technology of topical patches. A detailed discussion of their potential to overcome the limitations of existing therapies will then follow. Most importantly, to the best of our knowledge, this work unprecedentedly combines and discusses all the current advancements in innovative topical patches for the treatment of NMSC. In addition to this, the authors present our insights into the key considerations and emerging trends in the construction of these advanced topical patches. This review is meant for researchers and clinicians to consider utilising advanced topical patch systems in research and clinical trials toward localised interventions of NMSC. Full article

(This article belongs to the Special Issue Topical Drug Delivery: Current Status and Perspectives)

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