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Scientific Reports Jan 2024In our pursuit of enhancing acne treatment while minimizing side effects, we developed tailored Adapalene microsponges (MS) optimized using a Box-Behnken design 3. The...
In our pursuit of enhancing acne treatment while minimizing side effects, we developed tailored Adapalene microsponges (MS) optimized using a Box-Behnken design 3. The independent variables, Eudragit RS100 percentage in the polymer mixture, organic phase volume, and drug to polymer percentage, were explored. The optimized formulation exhibited remarkable characteristics, with a 98.3% ± 1.6 production yield, 97.3% ± 1.64 entrapment efficiency, and a particle size of 31.8 ± 1.1 µm. Notably, it achieved a 24 h cumulative drug release of 75.1% ± 1.4. To delve deeper into its efficacy, we evaluated the optimized microspongeal-gel in vitro, in vivo, and clinically. It demonstrated impressive retention in the pilosebaceous unit, a target for acne treatment. Comparative studies between our optimized Adapalene microspongeal gel and marketed Adapalene revealed superior performance. In vivo studies on Propionibacterium acnes-infected mice ears showed a remarkable 97% reduction in ear thickness, accompanied by a significant decrease in inflammatory signs and NF-κB levels, as confirmed by histopathological and histochemical examination. Moreover, in preliminary clinical evaluation, it demonstrated outstanding effectiveness in reducing comedonal lesions while causing fewer irritations. This not only indicates its potential for clinical application but also underscores its ability to enhance patient satisfaction, paving the way for future commercialization.
Topics: Humans; Mice; Animals; Adapalene; Acne Vulgaris; Skin; Polymers; Dermatologic Agents; Treatment Outcome; Gels
PubMed: 38228631
DOI: 10.1038/s41598-024-51392-1 -
American Journal of Ophthalmology Case... Mar 2022Periocular molluscum contagiosum can cause a chronic secondary follicular conjunctivitis or keratoconjunctivitis that rarely leads to corneal scarring and visual...
PURPOSE
Periocular molluscum contagiosum can cause a chronic secondary follicular conjunctivitis or keratoconjunctivitis that rarely leads to corneal scarring and visual impairment. We describe two cases of follicular conjunctivitis due to periocular molluscum contagiosum that were successfully treated with topical adapalene 0.1%.
OBSERVATIONS
Case 1 is a 9-year old female with a history of leg molluscum contagiosum who presented with three 1mm flesh-colored umbilicated papules on the periocular skin of the right eye with associated follicular conjunctivitis and diffuse corneal punctate epithelial erosions. Ocular symptoms were persistent for 6 months. Case 2 is a 4-year old female with a 3-month history of right periocular bumps and one month of conjunctival redness with eyelid edema. Examination revealed umbilicated flesh colored nodules on the right upper and lower eyelids with associated trace conjunctival injection. Both patients experienced rapid resolution of both eyelid involvement and conjunctivitis following the use of twice daily topical adapalene 0.1% to the eyelid lesions, with no reported side effects.
CONCLUSIONS AND IMPORTANCE
Topical adapalene 0.1% is a cost-effective, convenient, and non-toxic over-the-counter retinoid cream that should be considered for first-line therapy in the treatment of periocular molluscum contagiosum and any associated conjunctivitis.
PubMed: 35128166
DOI: 10.1016/j.ajoc.2022.101335 -
Materials Today. Bio Dec 2022Adapalene (AD) is an FDA-approved drug that shows good therapeutic efficacy for the treatment of acne vulgaris. However, due to its negative charge, AD cannot...
Adapalene (AD) is an FDA-approved drug that shows good therapeutic efficacy for the treatment of acne vulgaris. However, due to its negative charge, AD cannot efficiently penetrate across the also negatively-charged skin membrane. This study is the first to assess the treatment of acne vulgaris using electrostatically optimized AD emulsions prepared using anionic AD with methoxy polyethylene glycol--poly(ε-caprolactone) (MC) as an anionic emulsifier coupled with a newly synthesized MC with different contents of an amine pendant-group (MC-[NH]) as a cationic emulsifier. The AD emulsion prepared using MC-[NH] with high cationic charge potential was significantly stable in the short-term studies compared with anionic MC or no emulsifier. Furthermore, the AD emulsion prepared with the cationic MC-[NH] emulsifier provided a two or three times stronger therapeutic effect against acne vulgaris than the AD emulsion prepared with the anionic MC emulsifier or no emulsifier in an animal study. Additionally, the AD emulsion with high cationic charge potential exerted a remarkable inhibition of macrophage expression, as confirmed by histological analysis. Therefore, the electrostatic interaction between the negatively-charged skin membrane and the AD emulsion prepared with the cationic MC-[NH] emulsifier provides a promising therapeutic strategy for acne vulgaris.
PubMed: 35799897
DOI: 10.1016/j.mtbio.2022.100339 -
The Journal of Clinical and Aesthetic... Oct 2021Actinic keratoses (AKs) are sun-induced cutaneous lesions that may progress to squamous cell carcinoma (SCC). Photodynamic therapy (PDT) is an ideal treatment option for...
BACKGROUND
Actinic keratoses (AKs) are sun-induced cutaneous lesions that may progress to squamous cell carcinoma (SCC). Photodynamic therapy (PDT) is an ideal treatment option for AKs because it allows for treatment of field cancerization, selective destruction of diseased tissue, good cosmetic outcomes, and limited downtime.
OBJECTIVES
This study sought to determine the efficacy and safety of pretreating AKs of the dorsal hands and forearms with adapalene gel, an inexpensive and over-the-counter retinoid, prior to debridement of the target area and PDT with aminolevulinic hydrochloride acid (ALA, 10%) gel and narrowband red light.
METHODS
Fifteen patients with AK lesions of the right or left dorsal hands or forearms were pretreated with adapalene gel (0.1%) twice daily for one week prior to ALA-PDT. The other hand or forearm was treated with ALA-PDT (standard therapy), but not pretreated. For PDT, all treated areas were debrided with sandpaper, degreased with acetone, incubated for one hour with 10% ALA gel under occlusion, and illuminated with narrowband red light (~635 nm). All patients experienced one PDT treatment session.
RESULTS
Eight weeks after treatment, 12 subjects in the adapalene-pretreated group achieved 50% to 100% clearance compared to 10 subjects in the standard therapy group. The median lesion count reduction in the adapalene-pretreated group was -79% compared to -57% in the standard therapy group, and this difference was significant (=0.0164). The treatment was well-tolerated and the level of patient satisfaction was high.
CONCLUSIONS
Pretreatment with adapalene gel twice daily for one week may enhance efficacy in a single ALA-PDT treatment of AK lesions of the dorsal hand or forearm.
PubMed: 34976284
DOI: No ID Found -
The Journal of Histochemistry and... Nov 2019There is a growing recognition that myogenic stem cells are influenced by their microenvironment during regeneration. Several interstitial cell types have been described...
There is a growing recognition that myogenic stem cells are influenced by their microenvironment during regeneration. Several interstitial cell types have been described as supportive for myoblasts. In this role, both the pericyte as a possible progenitor for mesenchymal stem cells, and interstitial cells in the endomysium have been discussed. We have applied immunohistochemistry on normal and pathological human skeletal muscle using markers for pericytes, or progenitor cells and found a cell type co-expressing CD10, CD34, CD271, and platelet-derived growth factor receptor α omnipresent in the endomysium. The marker profile of these cells changed dynamically in response to muscle damage and atrophy, and they proliferated in response to damage. The cytology and expression profile of the CD10+ cells indicated a capacity to participate in myogenesis. Both morphology and indicated function of these cells matched properties of several previously described interstitial cell types. Our study suggests a limited number of cell types that could embrace many of these described cell types. Our study indicate that the CD10+, CD34+, CD271+, and platelet-derived growth factor receptor α+ cells could have a supportive role in human muscle regeneration, and thus the mechanisms by which they exert their influence could be implemented in stem cell therapy.
Topics: Adapalene; Antigens, CD34; Humans; Immunohistochemistry; Mesenchymal Stem Cells; Muscle, Skeletal; Neprilysin; Pericytes; Receptors, Platelet-Derived Growth Factor; Telocytes
PubMed: 31411936
DOI: 10.1369/0022155419871033 -
Cancer Science Aug 2022Various proteins are highly expressed in cancer (e.g., epidermal growth factor receptor); however, the majority are also expressed in normal cells, although they may...
Various proteins are highly expressed in cancer (e.g., epidermal growth factor receptor); however, the majority are also expressed in normal cells, although they may differ in expression intensity. Recently, we reported that CD271 (nerve growth factor receptor), a glycosylated protein, increases malignant behavior of cancer, particularly stemlike phenotypes in squamous cell carcinoma (SCC). CD271 is expressed in SCC and in normal epithelial basal cells. Glycosylation alterations generally occur in cancer cells; therefore, we attempted to establish a cancer-specific anti-glycosylated CD271 antibody. We purified recombinant glycosylated CD271 protein, immunized mice with the protein, and screened hybridomas using an ELISA assay with cancer cell lines. We established a clone G4B1 against CD271 which is glycosylated with O-glycan and sialic acid. The G4B1 antibody reacted with the CD271 protein expressed in esophageal cancer, but not in normal esophageal basal cells. This specificity was confirmed in hypopharyngeal and cervical cancers. G4B1 antibody recognized the fetal esophageal epithelium and Barrett's esophagus, which possess stem cell-like characteristics. In conclusion, G4B1 antibody could be useful for precise identification of dysplasia and cancer cells in SCC.
Topics: Adapalene; Animals; Antibodies, Monoclonal; Barrett Esophagus; Carcinoma, Squamous Cell; Esophageal Neoplasms; Glycosylation; Immunohistochemistry; Mice; Receptors, Nerve Growth Factor
PubMed: 35343032
DOI: 10.1111/cas.15340 -
Journal of Research in Medical Sciences... 2019Acne vulgaris (AV) is one of the most common skin diseases with major psychological impacts. Hence, selecting the best treatment modality is so important; there are...
BACKGROUND
Acne vulgaris (AV) is one of the most common skin diseases with major psychological impacts. Hence, selecting the best treatment modality is so important; there are different ways to treat AV such as topical and systemic agents, laser, and also photodynamic therapy. In this study, we tried to assess the difference between the efficacy of combination therapy with intense pulsed light (IPL) and benzoyl peroxide (BPO) in comparison with IPL and adapalene (AD) in the treatment of the mild to moderate AV.
MATERIALS AND METHODS
Thirty Iranian females in reproductive age with mild to moderate acne were enrolled in this study. The left and right side of the patients were randomized to receive either AD 0.1% or BPO 5% every other day plus three sessions of monthly apart IPL in the treatment of AV. Different parameters of AV such as acne severity index (ASI), total acne lesions counting (TLC), and Acne Global Severity Scale (AGSS) were measured before, during, and after the treatments.
RESULTS
There was a significant difference regarding AGSS, TLC, and ASI before and after treatment with AD plus IPL ( < 0.001). Furthermore, there was a significant difference regarding AGSS, TLC, and ASI before and after treatment with BP plus IPL ( < 0.001). However, no significant difference regarding AGSS, TLC, and ASI were observed between the 2 groups after treatment ( > 0.05). No significant side effects were observed in both groups.
CONCLUSION
Our study shows that there was not any significant difference between combining IPL with either AD or BPO so we can use either one of these combinations to achieve similar efficacy.
PubMed: 31850090
DOI: 10.4103/jrms.JRMS_398_19 -
The Oncologist Jul 2019The results of the APPEARANCE trial indicate that adapalene does not prevent acne-like rash over placebo when added to topical moisturizer and oral minocycline but... (Comparative Study)
Comparative Study Randomized Controlled Trial
Adapalene Gel 0.1% Versus Placebo as Prophylaxis for Anti-Epidermal Growth Factor Receptor-Induced Acne-Like Rash: A Randomized Left-Right Comparative Evaluation (APPEARANCE).
LESSONS LEARNED
The results of the APPEARANCE trial indicate that adapalene does not prevent acne-like rash over placebo when added to topical moisturizer and oral minocycline but instead may have a detrimental effect. Therefore, adapalene is not recommended as prophylaxis against acne-like rash induced by anti-epidermal growth factor receptor therapies.Given that acne-like rash was completely controlled with placebo in approximately half of patients, predictive measures to identify patients needing intensive prophylaxis are required.
BACKGROUND
Anti-epidermal growth factor receptor (EGFR) therapies are frequently associated with acne-like rash. To evaluate the prophylactic efficacy of adapalene, a topical retinoid used as first-line therapy for acne vulgaris, we conducted a randomized, placebo-controlled, evaluator-blinded, left-right comparative trial.
METHODS
Patients with non-small cell lung, colorectal, or head and neck cancer scheduled to receive anti-EGFR therapies were randomly assigned to once-daily adapalene application on one side of the face, with placebo on the other side. All patients had topical moisturizer coapplied to both sides of the face, and received oral minocycline. The primary endpoint was the difference in total facial lesion count of acne-like rash at 4 weeks. Secondary endpoints included complete control rate (CCR) of acne-like rash (≤5 facial lesions) and global skin assessment (Investigator's Global Assessment [IGA] scale, grade 0-4) at 4 weeks. Two blinded dermatologists independently evaluated the endpoints from photographs.
RESULTS
A total of 36 patients were enrolled, of whom 26 were evaluable. Adapalene treatment was associated with a greater lesion count than placebo at 4 weeks, although the difference was not statistically significant (mean, 12.6 vs. 9.8, = .12). All four patients with a difference >10 in lesion count between face sides had a greater count on the adapalene-treated side. No significant differences were observed in CCR of acne-like rash (54% vs. 50%) or IGA scale (mean grade, 1.9 vs. 1.7) between the adapalene and placebo sides.
CONCLUSION
Adapalene is not recommended as prophylaxis against acne-like rash induced by anti-EGFR therapies.
Topics: Acne Vulgaris; Adapalene; Aged; Aged, 80 and over; Carcinoma, Non-Small-Cell Lung; Colorectal Neoplasms; Dermatologic Agents; ErbB Receptors; Exanthema; Female; Follow-Up Studies; Gels; Head and Neck Neoplasms; Humans; Lung Neoplasms; Male; Middle Aged; Prognosis; Protein Kinase Inhibitors
PubMed: 30890624
DOI: 10.1634/theoncologist.2019-0156 -
Cureus Jan 2023Lichen planus pigmentosus (LPP) is a rare variant of lichen planus. Due to the scarce number of patients diagnosed with LPP, there are no treatment guidelines. Multiple...
Lichen planus pigmentosus (LPP) is a rare variant of lichen planus. Due to the scarce number of patients diagnosed with LPP, there are no treatment guidelines. Multiple topical and oral agents are utilized in LPP with varying degrees of response. Isotretinoin has only been investigated in a case report and a single prospective pilot study for managing LPP. Herein, we report the efficacy, safety, and moderate improvement of LPP patients on isotretinoin 20 mg (0.25 mg/kg), topical adapalene gel, 4% hydroquinone cream, and topical sunscreen.
PubMed: 36741605
DOI: 10.7759/cureus.33255 -
Journal of Personalized Medicine Dec 2022Homeostasis in the differentiation programme of sebaceous stem cells has been identified as a key step in comedogenesis and should be a target for acne-prone skin care.
BACKGROUND
Homeostasis in the differentiation programme of sebaceous stem cells has been identified as a key step in comedogenesis and should be a target for acne-prone skin care.
OBJECTIVE
To report on a multicentre, year-long/real-life use study of a patented natural product containing proven to modulate molecular actors in the initial steps of comedogenesis.
METHODS
An open-label multicentric international study, with a 12 month follow-up, included 54 teenage and young adult subjects with mild to moderate facial acne. The study was aimed at reproducing a real-life use context.
RESULTS
Total lesion count mean was 88.3 at inclusion. There was a sustained, highly significant decrease over the months of clinical lesion counts (45.6% improvement after 6 months and 59.6% at 12 months) and on other efficacy markers, associated with a significant decrease in global microcomedone quantity on cyanoacrylate superficial skin surface biopsies. Importantly, the study protocol allowed the dermatologist to prescribe, if needed as in real life, any of the acne drugs registered in the acne guidelines. The exposure to these acne drugs during the whole year was calculated as a percentage of /352 days of use and happened to be very limited at less than 4%, which indicates a marginal contribution to the sustained clinical improvement. (Oral and local acne treatments: Lymecycline 1.46%; Doxycycline 0.24%; Adapalene 0.16% or gel association with Benzoyl peroxide 1.17%; Clindamycin 0.04%; Benzoyl peroxide 1.5%; Erythromycin 0.75%). The tolerance with daily long-term use was good.
LIMITATIONS
The association with routine prescription acne drugs when needed, even if limited, does not allow a full evaluation of the intrinsic quantitative efficacy of in lesion reduction.
CONCLUSION
This open, real-life, year-long multicentre study confirms a previous 48-week proof of concept study and qualifies the use of as a "field-dermo cosmetic" contributing to homeostasis of acne-prone skin in association with acne drugs.
PubMed: 36675757
DOI: 10.3390/jpm13010096