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1.
Arch Dermatol Res ; 316(7): 350, 2024 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-38850408

RESUMO

Loss and absence of melanocytes due to a number of factors is responsible for vitiligo; known to be the commonest disorder of pigmentation. The aim of the current work was to compare the efficacy and safety of excimer light with topical tacrolimus ointment 0.1% versus excimer light with topical bimatoprost gel 0.01% in treatment of facial vitiligo. The study was carried out on 48 patients presented with facial vitiligo. The patients were divided randomly using sealed envelope method into two groups (24 patients each). Group 1 were treated with excimer light plus topical tacrolimus ointment 0.1% and group 2 treated with excimer light plus topical bimatoprost gel 0.01%. Clinical improvement based on the quartile grading scale at the end of treatment did not show any statistically significant difference between groups. The majority of subjects in both groups experienced good to excellent improvement. Only 20.9% of patients in group 1 and 33.3% of subjects in group 2 achieved less than 50% repigmentation (p = 0.889). Our study demonstrated that 0.01% topical bimatoprost gel in combination with excimer light is considered safe and effective as treatment of nonsegmental facial vitiligo with comparable results to 0.1% tacrolimus.


Assuntos
Bimatoprost , Tacrolimo , Vitiligo , Humanos , Vitiligo/tratamento farmacológico , Vitiligo/terapia , Vitiligo/diagnóstico , Tacrolimo/administração & dosagem , Bimatoprost/administração & dosagem , Feminino , Masculino , Adulto , Resultado do Tratamento , Adulto Jovem , Adolescente , Pessoa de Meia-Idade , Lasers de Excimer/uso terapêutico , Administração Tópica , Pigmentação da Pele/efeitos dos fármacos , Pigmentação da Pele/efeitos da radiação , Face , Administração Cutânea , Criança , Terapia Combinada/métodos , Imunossupressores/administração & dosagem , Imunossupressores/uso terapêutico
2.
Clin Ophthalmol ; 18: 1371-1377, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38765460

RESUMO

Purpose: To characterize clinical outcomes following a single administration of bimatoprost SR in eyes with glaucoma in a real-world setting implanted at the slit-lamp. Setting: Tertiary care Glaucoma practice, Glaucoma Associates of Texas, Dallas, Texas. Design: Retrospective interventional case series. Methods: Data were analyzed from consecutive patients receiving a single bimatoprost SR implant from the time of its approval to the time of data collection. All eyes were implanted at the slit-lamp. Eyes with less than 1 month of follow-up were excluded. The primary outcome was median time to next intraocular pressure (IOP)-lowering intervention. Mean IOP and medication use, and changes from baseline, were also assessed through 12 months of follow-up. Results: Overall 129 eyes of 81 patients were analyzed. Following bimatoprost SR administration (replacing a topical prostaglandin analogue [PGA] in most eyes), the median survival time without any further IOP-lowering interventions was between 6-9 months. Mean IOP remained unchanged from baseline at month 1 (consistent with switch from topical to intracameral PGA therapy) and began to rise at month 3. At month 12, 40.5% of eyes (52 eyes) remained intervention-free, mean medication reduction was 0.5 medications per eye, and 27.8% of eyes (36 eyes) were medication-free. Adverse events were uncommon and most were transient and resolved with or without intervention. Conclusion: This real-world analysis of bimatoprost SR use for glaucoma therapy complements Phase 3 study findings and demonstrates that the implant can safely provide medication reduction through 6 months in most eyes and through 12 months in almost 40% of eyes.

3.
Pharmaceuticals (Basel) ; 17(5)2024 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-38794131

RESUMO

BACKGROUND: Bimatoprost has emerged as a significant medication in the field of medicine over the past several decades, with diverse applications in ophthalmology, dermatology, and beyond. Originally developed as an ocular hypotensive agent, it has proven highly effective in treating glaucoma and ocular hypertension. Its ability to reduce intraocular pressure has established it as a first-line treatment option, improving management and preventing vision loss. In dermatology, bimatoprost has shown promising results in the promotion of hair growth, particularly in the treatment of alopecia and hypotrichosis. Its mechanism of action, stimulating the hair cycle and prolonging the growth phase, has led to the development of bimatoprost-containing solutions for enhancing eyelash growth. AIM: The aim of our review is to provide a brief description, overview, and studies in the current literature regarding the versatile clinical use of bimatoprost in recent years. This can help clinicians determine the most suitable individualized therapy to meet the needs of each patient. METHODS: Our methods involve a comprehensive review of the latest advancements reported in the literature in bimatoprost formulations, which range from traditional eye drops to sustained-release implants. These innovations offer extended drug delivery, enhance patient compliance, and minimize side effects. RESULTS: The vast literature published on PubMed has confirmed the clinical usefulness of bimatoprost in lowering intraocular pressure and in managing patients with glaucoma. Numerous studies have shown promising results in dermatology and esthetics in promoting hair growth, particularly in treating alopecia and hypotrichosis. Its mechanism of action involves stimulating the hair cycle and prolonging the growth phase, leading to the development of solutions that enhance eyelash growth. The global use of bimatoprost has expanded significantly, with applications growing beyond its initial indications. Ongoing research is exploring its potential in glaucoma surgery, neuroprotection, and cosmetic procedures. CONCLUSIONS: Bimatoprost has shown immense potential for addressing a wide range of therapeutic needs through various formulations and advancements. Promising future perspectives include the exploration of novel delivery systems such as contact lenses and microneedles to further enhance drug efficacy and patient comfort. Ongoing research and future perspectives continue to shape its role in medicine, promising further advancements and improved patient outcomes.

4.
Cureus ; 16(3): e56233, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38618411

RESUMO

Background and objective Bimatoprost ophthalmic solution (0.03%) is used for the treatment of ocular hypertension. However, one of the side effects of this prescription is that it causes overgrowth of eyelashes, causing hypertrichosis. Therefore, the Bimatoprost ophthalmic solution was rebranded to be used for cosmetic purposes. This study aims to assess the awareness and practices of female university students regarding the use of Careprost (Bimatoprost, Latisse, Allergan, Inc., Irvine, CA) for cosmetic purposes. Methodology A descriptive cross-sectional study was conducted among female students at Bisha University, including those from medical and non-medical colleges, spanning from November 2022 to February 2023. All participants who completed the study questionnaire were considered for analysis, but those who had missing answers were excluded from the study. The total number of participants was 305, representing an 81.2% response rate out of the 376 surveys distributed. Results A total of 305 students completed the survey, with approximately 132 (54.5%) from the medical college and 173 (65.3%) from the non-medical college. Approximately 32 (24.2%) of participants from the medical college and 51 (29.4%) from the non-medical college understood that Bimatoprost drops can be used for the elongation of eyelashes. More than half of the participants were not aware of the side effects of Careprost (0.03%), including 65 (49.2%) medical students and 108 (62.7%) non-medical students. In total, 42 (13.77%) of the participants believed that Careprost (0.03%) could be administered without a prescription. Among the participants, 75 (24.59%) reported that they had previously used Careprost (0.03%) eye drops. Additionally, more than one-fourth of the participants (83, 27.2%) thought that Careprost (0.03%) could be used for eyelash elongation. Conclusions This study revealed that female university students had a poor level of awareness and practices about the cosmetic uses of Careprost (0.03%) eye drops for eyelashes. A better awareness level was noted regarding the side effects of Careprost drops, which may have contributed to a low utilization rate among female students.

5.
Eur J Ophthalmol ; 34(4): NP20-NP24, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38619930

RESUMO

PURPOSE: This case report aims to report the development of cystoid macular edema (CME) unilaterally following the administration of bimatoprost implant (Durysta) injections in both eyes for the treatment of primary open-angle glaucoma (POAG). OBSERVATIONS: An 84-year-old female patient, previously diagnosed with POAG, underwent bimatoprost implant (Durysta) injections in both eyes, spaced one month apart. Subsequently, the patient experienced a gradual decline in visual acuity in her left eye attributed to the development of CME. The condition resolved following a treatment regimen involving topical dexamethasone and nepafenac. CONCLUSION: The use of bimatoprost implant may lead to the occurrence of CME. Ophthalmologists must vigilantly monitor patients post-implantation, especially if they exhibit visual symptoms or have risk factors for a CME.


Assuntos
Anti-Hipertensivos , Bimatoprost , Implantes de Medicamento , Glaucoma de Ângulo Aberto , Pressão Intraocular , Edema Macular , Tomografia de Coerência Óptica , Acuidade Visual , Humanos , Edema Macular/diagnóstico , Edema Macular/tratamento farmacológico , Feminino , Bimatoprost/efeitos adversos , Glaucoma de Ângulo Aberto/tratamento farmacológico , Glaucoma de Ângulo Aberto/cirurgia , Idoso de 80 Anos ou mais , Pressão Intraocular/efeitos dos fármacos , Implantes de Medicamento/efeitos adversos , Anti-Hipertensivos/efeitos adversos , Glucocorticoides/administração & dosagem , Glucocorticoides/efeitos adversos , Glucocorticoides/uso terapêutico , Câmara Anterior , Dexametasona/administração & dosagem , Dexametasona/efeitos adversos
6.
Int J Pharm X ; 7: 100240, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38577618

RESUMO

Bimatoprost (BIM) is a prostaglandin F2α analogs originally approved for the treatment of glaucoma and ocular hypertension. Recent studies have highlighted its potential to boost hair growth. The objective of this investigation is to challenge the potential of spanlastics (SLs) as a surfactant-based vesicular system for promoting the cutaneous delivery of BIM for the management of alopecia. BIM-loaded spanlastics (BIM-SLs), composed of Span as the main vesicle component and Tween as the edge activator, were fabricated by ethanol injection method. The formulated BIM-SLs were optimized by 23 full factorial design. The optimized formula (F1) was characterized for entrapment efficiency, surface charge, vesicle size, and drug release after 12 h (Q12h). The optimized formula (F1) exhibited high drug entrapment efficiency (83.1 ± 2.1%), appropriate zeta potential (-19.9 ± 2.1 mV), Q12h of 71.3 ± 5.3%, and a vesicle size of 364.2 ± 15.8 nm, which favored their cutaneous accumulation. In addition, ex-vivo skin deposition studies revealed that entrapping BIM within spanlastic-based nanogel (BIM-SLG) augmented the dermal deposition of BIM, compared to naïve BIM gel. Furthermore, in vivo studies verified the efficacy of spanlastic vesicles to boost the cutaneous accumulation of BIM compared to naive BIM gel; the AUC0-12h of BIM-SLG was 888.05 ± 72.31 µg/mL.h, which was twice as high as that of naïve BIM gel (AUC0-12h 382.86 ± 41.12 µg/mL.h). Intriguingly, BIM-SLG outperforms both naïve BIM gel and commercial minoxidil formulations in stimulating hair regrowth in an androgenetic alopecia mouse model. Collectively, spanlastic vesicles might be a potential platform for promoting the dermal delivery of BIM in managing alopecia.

7.
Med Eng Phys ; 124: 104110, 2024 02.
Artigo em Inglês | MEDLINE | ID: mdl-38418021

RESUMO

Drug-eluting contact lenses (DECLs) incorporated with poly(lactic-co-glycolic acid) (PLGA) and various model drugs (ketotifen fumarate, bimatoprost and latanoprost) were fabricated using nanoelectrospray (nES) approach. The resulting DECLs demonstrated outstanding optical transmittance within the optical zone, indicating that the employed coating procedure did not compromise visual acuity under the prescribed spraying parameters. In vitro drug release assessments of the model drugs (ketotifen fumarate (KF), bimatoprost (BIM), and latanoprost (LN)) revealed a strong correlation between the model drug's hydrophobicity and the duration of drug release. Changing the drug loading of the more hydrophilic model drugs, BIM and KF, showed no impact on the drug release kinetics of DECLs loaded with BIM and KF. However, for the hydrophobic model drug, LN, the highest LN loading led to the most extended drug release. The conventional steam sterilisation method was found to damage the PLGA coating on the DECLs fabricated by nES. An alternative sterilisation strategy, such as radiation sterilisation may need to be investigated in the future study to minimise potential harm to the coating.


Assuntos
Lentes de Contato , Cetotifeno , Latanoprosta , Cetotifeno/química , Bimatoprost , Sistemas de Liberação de Medicamentos
8.
J Cosmet Dermatol ; 23(5): 1663-1668, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38321929

RESUMO

BACKGROUND: Transepidermal drug delivery is a novel therapeutic technique to boost efficacy of topical drugs. AIM: In this clinical trial we evaluate the efficacy of the combination of fractional carbon dioxide (FCO2) laser and bimatoprost solution compared to bimatoprost alone in the treatment of alopecia areata. METHODS: This is a prospective intra-patient comparative randomized clinical trial on 20 patients with alopecia areata. In each participant two patches were chosen to randomly receive either topical 0.03% bimatoprost solution (twice a day for 12 weeks) alone or in combination with FCO2 laser (every 2 weeks for 12 weeks). Then response to treatment was evaluated by the measurement of the severity of alopecia tool score system (SALT) score, percentage of hair regrowth, physician assessment and patients' satisfaction. RESULTS: SALT score was reduced significantly during treatment sessions and after a 3-month follow-up in both treatment groups (p = 0.000). The mean percentage of improvement in SALT score in the combination therapy and monotherapy groups were 46.43 ± 4.35% and 21.16 ± 4.06% at the end of the study and 46.42 ± 5.75% and16.11 ± 3.10% at the end of the follow-up period, respectively (p = 0.000). A general linear model of two-way analysis demonstrated a significantly superior outcome in the combination therapy group compared to the monotherapy group during time (F1.6, 13.2 = 43.8. p = 0.000). CONCLUSION: Fractional ablative laser can be considered as an assistant method for enhancing of efficacy of topical drugs especially in refractory cases of patchy alopecia areata.


Assuntos
Alopecia em Áreas , Bimatoprost , Lasers de Gás , Satisfação do Paciente , Humanos , Alopecia em Áreas/tratamento farmacológico , Alopecia em Áreas/terapia , Bimatoprost/administração & dosagem , Adulto , Feminino , Masculino , Lasers de Gás/uso terapêutico , Estudos Prospectivos , Terapia Combinada/métodos , Adulto Jovem , Resultado do Tratamento , Índice de Gravidade de Doença , Administração Cutânea , Pessoa de Meia-Idade , Adolescente , Cabelo/efeitos dos fármacos , Cabelo/crescimento & desenvolvimento , Sistemas de Liberação de Medicamentos/métodos
9.
Ophthalmol Ther ; 13(1): 71-92, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37737923

RESUMO

INTRODUCTION: Sustained-release intraocular implants provide a therapeutic option for open-angle glaucoma (OAG) and ocular hypertension (OHT) patients who are non-compliant with eyedrops. Currently, there are no published patient-reported outcome (PRO) measures that assess treatment satisfaction with intraocular implants. To address this gap, a new PRO instrument, the Allergan Satisfaction with Treatment Experience Questionnaire (ASTEQ), has been developed in accordance with Food and Drug Administration guidance. METHODS: Qualitative research interviews were conducted among patients with OAG/OHT who had received three intraocular injections of a sustained-release bimatoprost (10 or 15 µg) implant within the clinical trial setting. A preliminary conceptual framework capturing treatment satisfaction concepts in glaucoma, as identified from the literature, was used to develop a semi-structured interview guide. A concept elicitation (CE) interview to identify aspects of the glaucoma treatment experience pertinent to intraocular implants provided content for a draft instrument. A cognitive debriefing (CD) interview to test the instrument's interpretability, relevance, and validity informed its subsequent refinement. Interview analysis followed a grounded theory approach to identify data patterns and relationships. RESULTS: CE interviews (n = 19) indicated that participants' main considerations in rating satisfaction with implant treatment were physical comfort during preparation for the implant and implant administration, anxiety about the procedure, frequency of implant administration, possible side effects, convenience and accessibility of the implant, relationship with the clinician, and lifestyle fit. Draft ASTEQ revision based on CD interviews (n = 20) and readability tests yielded a nine-item ASTEQ instrument comprising satisfaction with overall implant experience and frequency of administration, occurrence/bother of immediate and long-term side effects, worry about implant administration and possible risks/side effects, and physical discomfort during preparation for the implant and implant administration. CONCLUSION: The ASTEQ instrument has demonstrated content validity in patients with OAG/OHT treated with a sustained-release bimatoprost implant. Further research is necessary to evaluate its psychometric properties.

10.
J Fr Ophtalmol ; 47(2): 103996, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-37926661

RESUMO

The present retrospective study evaluated intraocular pressure (IOP) and medication burden after bimatoprost sustained-release (bimatoprost SR, Durysta, Allergan) implantation in patients with glaucoma. A secondary objective was to examine an effect of bimatoprost SR in a subset of patients with prior minimally invasive and incisional glaucoma surgery. A retrospective chart review of 122 eyes that received bimatoprost SR by 6 glaucoma specialists at Wills Eye Hospital between March 2020 and September 2021 was performed. One hundred and eighteen eyes from 84 patients had a reduction in IOP (18.5±5.7mmHg vs. 16.0±5.4mmHg, P<0.01) and required fewer glaucoma medications (2.1±1.4 vs. 1.2±1.2, P<0.01) after bimatoprost SR implantation. In 41 eyes from 31 patients who previously underwent glaucoma surgery (including iStent, goniotomy, trabeculectomy, Xen Gel Stent, or tube shunt surgery), medication burden was decreased after bimatoprost SR implantation (1.9±1.3 vs. 1.0±1.0, P<0.001). These data suggest that bimatoprost SR is an efficacious treatment modality for glaucoma, even in post-surgical patients.


Assuntos
Glaucoma , Pressão Intraocular , Humanos , Bimatoprost/efeitos adversos , Estudos Retrospectivos , Preparações de Ação Retardada/uso terapêutico , Glaucoma/tratamento farmacológico , Glaucoma/cirurgia , Glaucoma/induzido quimicamente , Resultado do Tratamento
11.
Graefes Arch Clin Exp Ophthalmol ; 262(1): 179-190, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37615697

RESUMO

PURPOSE   : To compare the efficacy and safety of the fixed-dose combination (FDC) of netarsudil 0.02%/latanoprost 0.005% ophthalmic solution (NET/LAT; Roclanda®) with bimatoprost 0.03%/timolol maleate 0.5% (BIM/TIM; Ganfort®) ophthalmic solution in the treatment of open-angle glaucoma (OAG) and ocular hypertension (OHT). METHODS: MERCURY-3 was a 6-month prospective, double-masked, randomized, multicenter, active-controlled, parallel-group, non-inferiority study. Patients (≥ 18 years) with a diagnosis of OAG or OHT in both eyes that was insufficiently controlled with topical medication (IOP ≥ 17 mmHg in ≥ 1 eye and < 28 mmHg in both eyes) were included. Following washout, patients were randomized to once-daily NET/LAT or BIM/TIM for up to 6 months; efficacy was assessed at Week 2, Week 4, and Month 3; safety was evaluated for 6 months. Comparison of NET/LAT relative to BIM/TIM for mean IOP at 08:00, 10:00, and 16:00 h was assessed at Week 2, Week 6, and Month 3. Non-inferiority of NET/LAT to BIM/TIM was defined as a difference of ≤ 1.5 mmHg at all nine time points through Month 3 and ≤ 1.0 mmHg at five or more of nine time points through Month 3. RESULTS: Overall, 430 patients were randomized (NET/LAT, n = 218; BIM/TIM, n = 212), and all received at least one dose of study medication. Efficacy analyses were performed at Month 3 on 388 patients (NET/LAT, n = 184; BIM/TIM, n = 204). NET/LAT demonstrated non-inferiority to BIM/TIM, with a between-treatment difference in IOP of ≤ 1.5 mmHg achieved at all time points and ≤ 1.0 mmHg at the majority of time points (six of nine) through Month 3. Mean diurnal IOP during the study ranged from 15.4 to 15.6 mmHg and 15.2 to 15.6 mmHg in the NET/LAT and BIM/TIM groups respectively, with no between-group statistically significant difference. No significant differences were observed in key secondary endpoints. No serious, treatment-related adverse events (AEs) were observed, and AEs were typically mild/moderate in severity. The most common treatment-related AEs were conjunctival hyperemia (NET/LAT, 30.7%; BIM/TIM, 9.0%) and cornea verticillata (NET/LAT, 11.0%; BIM/TIM, 0%). CONCLUSIONS: Once-daily NET/LAT was non-inferior to BIM/TIM in IOP reduction in OAG and OHT, with AEs consistent with previous findings. NET/LAT offers a compelling alternative FDC treatment option for OAG and OHT.


Assuntos
Benzoatos , Glaucoma de Ângulo Aberto , Hipertensão Ocular , beta-Alanina/análogos & derivados , Humanos , Glaucoma de Ângulo Aberto/diagnóstico , Glaucoma de Ângulo Aberto/tratamento farmacológico , Timolol/efeitos adversos , Bimatoprost/uso terapêutico , Latanoprosta/efeitos adversos , Estudos Prospectivos , Pressão Intraocular , Anti-Hipertensivos/efeitos adversos , Tonometria Ocular , Hipertensão Ocular/diagnóstico , Hipertensão Ocular/tratamento farmacológico , Soluções Oftálmicas , Resultado do Tratamento , Método Duplo-Cego
12.
Polymers (Basel) ; 15(21)2023 Nov 06.
Artigo em Inglês | MEDLINE | ID: mdl-37960016

RESUMO

This study aimed at formulating the antiglaucoma agent, Bimatoprost (BMT), into niosomal in situ gel (BMT-ISG) for ocular delivery. Niosomes containing cholesterol/span 60 entrapping BMT were fabricated using a thin-film hydration method. The fabricated niosomes were optimized and characterized for entrapment efficiency (%EE) and size. The optimized BMT-loaded niosomal formulation prepared at a cholesterol/span 60 ratio of 1:2 exhibited the highest entrapment (81.2 ± 1.2%) and a small particle size (167.3 ± 9.1 nm), and they were selected for incorporation into in situ gelling systems (BMT-ISGs) based on Pluronic F127/Pluronic F68. Finally, the in vivo efficiency of the BMT-ISG formulation, in terms of lowering the intraocular pressure (IOP) in normotensive male albino rabbits following ocular administration, was assessed and compared to that of BMT ophthalmic solution. All the formulated BMT-ISGs showed sol-gel transition temperatures ranging from 28.1 °C to 40.5 ± 1.6 °C. In addition, the BMT-ISG formulation sustained in vitro BMT release for up to 24 h. Interestingly, in vivo experiments depicted that topical ocular administration of optimized BMT-ISG formulation elicited a significant decline in IOP, with maximum mean decreases in IOP of 9.7 ± 0.6 mm Hg, compared to BMT aqueous solution (5.8 ± 0.6 mm Hg). Most importantly, no signs of irritation to the rabbit's eye were observed following topical ocular administration of the optimized BMT-ISG formulation. Collectively, our results suggested that niosomal in situ gels might be a feasible delivery vehicle for topical ocular administration of anti-glaucoma agents, particularly those with poor ocular bioavailability.

13.
Biomed Pharmacother ; 168: 115446, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37918255

RESUMO

Colistin (polymyxin E) is an antibiotic that is effective against multidrug-resistant gram-negative bacteria. However, the high incidence of nephrotoxicity caused by colistin limits its clinical use. To identify compounds that might ameliorate colistin-induced nephrotoxicity, we obtained 1707 compounds from the Korea Chemical Bank and used a high-content screening (HCS) imaging-based assay. In this way, we found that bimatoprost (one of prostaglandin F2α analogue) ameliorated colistin-induced nephrotoxicity. To further assess the effects of bimatoprost on colistin-induced nephrotoxicity, we used in vitro and in vivo models. In cultured human proximal tubular cells (HK-2), colistin induced dose-dependent cytotoxicity. The number of terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL)-positive cells, indicative of apoptosis, was higher in colistin-treated cells, but this effect of colistin was ameliorated by cotreatment with bimatoprost. The generation of reactive oxygen species, assessed using 2,7-dichlorodihydrofluorescein diacetate, was less marked in cells treated with both colistin and bimatoprost than in those treated with colistin alone. Female C57BL/6 mice (n = 10 per group) that were intraperitoneally injected with colistin (10 mg/kg/12 hr) for 14 days showed high blood urea nitrogen and serum creatinine concentrations that were reduced by the coadministration of bimatoprost (0.5 mg/kg/12 hr). In addition, kidney injury molecule-1 (KIM1) and Neutrophil gelatinase-associated lipocalin (NGAL) expression also reduced by bimatoprost administration. Further investigation in tubuloid and kidney organoids also showed that bimatoprost attenuated the nephrotoxicity by colistin, showing dose-dependent reducing effect of KIM1 expression. In this study, we have identified bimatoprost, prostaglandin F2α analogue as a drug that ameliorates colistin-induced nephrotoxicity.


Assuntos
Colistina , Dinoprosta , Camundongos , Animais , Feminino , Humanos , Colistina/farmacologia , Bimatoprost/metabolismo , Bimatoprost/farmacologia , Dinoprosta/metabolismo , Camundongos Endogâmicos C57BL , Antibacterianos/toxicidade , Rim , Prostaglandinas/metabolismo
14.
Nanomedicine (Lond) ; 2023 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-37991004

RESUMO

Background: Bimatoprost is a drug used to lower intraocular pressure in the treatment of glaucoma. Conventional eye drops have the limitations of repeated dosing, drug loss due to tear outflow and hence poor availability for action. Materials & methods: Using a systematic quality by design approach, liposomes and solid lipid nanoparticles were formulated and further encapsulated in thermo-sensitive in situ hydrogel. Results & conclusion: Optimized liposomes had 87.04% encapsulation efficiency and 306.78 nm mean particle size, while solid lipid nanoparticles had 90.51% and 304.21 nm. Bimatoprost liposomes had controlled zero-order drug kinetics and no initial burst release, making them better than solid lipid nanoparticles. Bimatoprost-loaded liposomes in thermo-sensitive hydrogel decreased intraocular pressure for 18 h.

15.
J Lipid Res ; 64(11): 100444, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37730163

RESUMO

White adipose tissue regulation is key to metabolic health, yet still perplexing. The chief endocannabinoid anandamide metabolite, prostaglandin F2α ethanolamide (PGF2αEA), inhibits adipogenesis, that is, the formation of mature adipocytes. We observed that adipocyte progenitor cells-preadipocytes-following treatment with PGF2αEA yielded larger pellet sizes. Thus, we hypothesized that PGF2αEA might augment preadipocyte proliferation. Cell viability MTT and crystal violet assays, cell counting, and 5-bromo-2'-deoxyuridine incorporation in cell proliferation ELISA analyses confirmed our prediction. Additionally, we discovered that PGF2αEA promotes cell cycle progression through suppression of the expression of cell cycle inhibitors, p21 and p27, as shown by flow cytometry and qPCR. Enticingly, concentrations of this compound that showed no visible effect on cell proliferation or basal transcriptional activity of peroxisome proliferator-activated receptor gamma could, in contrast, reverse the anti-proliferative and peroxisome proliferator-activated receptor gamma-transcription activating effects of rosiglitazone (Rosi). MTT and luciferase reporter examinations supported this finding. The PGF2αEA pharmaceutical analog, bimatoprost, was also investigated and showed very similar effects. Importantly, we suggest the implication of the mitogen-activated protein kinase pathway in these effects, as they were blocked by the selective mitogen-activated protein kinase kinase inhibitor, PD98059. We propose that PGF2αEA is a pivotal regulator of white adipose tissue plasticity, acting as a regulator of the preadipocyte pool in adipose tissue.


Assuntos
Endocanabinoides , PPAR gama , Camundongos , Animais , Endocanabinoides/farmacologia , PPAR gama/genética , PPAR gama/metabolismo , Adipogenia , Proliferação de Células , Prostaglandinas , Células 3T3-L1 , Diferenciação Celular
16.
J Clin Aesthet Dermatol ; 16(9): 28-32, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37720195

RESUMO

Background: Hypopigmented scars are challenging to treat due to a lack of effective treatments and often transient results. Recent reports suggest that prostaglandin analog-induced hyperpigmentation may have favorable dermatological applications. Objective: Analyze previous studies involving the use of prostaglandin analogs in the treatment of hypopigmented scars. Methods: PubMed/Medline was queried through 10/01/2022 with the following search terms: (bimatoprost AND scar), (latanoprost AND scar), (travoprost AND scar), (prostaglandin analogs AND hypopigmented scars), (PGF2alpha AND hyperpigmentation), (prostaglandin analogs AND hyperpigmentation). Results: In total, 88 unique studies were reviewed for eligibility. Five studies met inclusion criteria including two prospective, double-blinded, randomized (only one was placebo-controlled), one prospective case series, one retrospective chart review, and one case report; comprising a total of 87 patients. All five studies utilized topical prostaglandin analogs as an adjunctive treatment via laser-assisted delivery. While both, the placebo-controlled and non-placebo-controlled, trials reported more than 75 percent of patients experienced at least 50 percent or more (Grade 3 or higher) improvement, the retrospective study reported 100 percent of patients experienced at least 75 percent or more (Grade 4 or higher) improvement, measured as scar repigmentation. The prospective case series and the reported single case showed overall qualitative improvement in all patients measured as repigmentation of hypopigmented and depigmented scars. Limitations: Different laser devices, parameters, treatment frequency, and follow-up timepoints. Conclusion: All studies evaluated demonstrated favorable treatment outcomes with no reported adverse events. Additional, large randomized controlled trials are needed to fully assess the effectiveness and long-term safety of PGF2α agonists for hypopigmented scars.

17.
Arch Dermatol Res ; 315(9): 2635-2641, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37517060

RESUMO

Eyebrows are an important feature of facial identity and communications in human beings as well as an important eye defense shield from dust and foreign bodies. To compare the efficacy and safety between 0.01%, 0.03% bimatoprost and minoxidil 2% in gel formulations for eyebrow enhancement. Sixty eligible subjects were female or male, aged 18 years or older with eyebrow hypotrichosis, defined as either a Grade 1 or 2 on the Global Eyebrow Assessment (GEBA) scale. Patients were randomized into 3 groups using block randomization. Group a (20 patients) applied topical 0.03% bimatoprost gel once daily onto both eyebrows, group b (20 patients) applied topical 0.01% bimatoprost gel once daily onto both eyebrows while group c (20 patients) applied topical minoxidil 2% gel once daily onto both eyebrows. A significant improvement in GEBA score was reported in all the three groups after treatment (P ≤ 0.001); however, there was no statistically significant difference between the three groups (P1 = 0.091; P2 = 0.102; P3 = 0.663). Bimatoprost is equally efficacious as minoxidil in enhancement of eyebrows with a more favorable response produced by the 0.03% concentration.


Assuntos
Hipotricose , Minoxidil , Humanos , Masculino , Feminino , Bimatoprost/efeitos adversos , Minoxidil/efeitos adversos , Sobrancelhas , Hipotricose/tratamento farmacológico , Administração Tópica , Resultado do Tratamento , Método Duplo-Cego
18.
Pharmaceuticals (Basel) ; 16(7)2023 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-37513913

RESUMO

Glaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer from relatively low ocular bioavailability. The objective of this study was to fabricate and optimize solid lipid nanoparticles (SLNs) containing Bimatoprost for ocular administration for the management of glaucoma. Bimatoprost-loaded SLNs were fabricated by solvent evaporation/ultrasonication technique. Glyceryl Monostearate (GMS) was adopted as solid lipid and poloxamer 407 as surfactant. Optimization of SLNs was conducted by central composite design. The optimized formulation was assessed for average particle size, entrapment efficiency (%), zeta potential, surface morphology, drug release study, sterility test, isotonicity test, Hen's egg test-chorioallantoic membrane (HET-CAM) test and histopathology studies. The optimized Bimatoprost-loaded SLNs formulation had an average size of 183.3 ± 13.3 nm, zeta potential of -9.96 ± 1.2 mV, and encapsulation efficiency percentage of 71.8 ± 1.1%. Transmission electron microscopy (TEM) study revealed the nearly smooth surface of formulated particles with a nano-scale size range. In addition, SLNs significantly sustained Bimatoprost release for up to 12 h, compared to free drug (p < 005). Most importantly, HET-CAM test nullified the irritancy of the formulation was verified its tolerability upon ocular use, as manifested by a significant reduction in mean irritation score, compared to positive control (1% sodium dodecyl sulfate; p < 0.001). Histopathology study inferred the absence of any signs of cornea tissue damage upon treatment with Bimatoprost optimized formulation. Collectively, it was concluded that SLNs might represent a viable vehicle for enhancing the corneal permeation and ocular bioavailability of Bimatoprost for the management of glaucoma.

19.
J Ocul Pharmacol Ther ; 39(6): 398-403, 2023 07.
Artigo em Inglês | MEDLINE | ID: mdl-37389843

RESUMO

Purpose: Sustained intraocular drug delivery devices are being developed to lower intraocular pressure (IOP) and improve adherence in patients with glaucoma. The purpose of this study was to assess the IOP and eyedrop usage reduction effects of intracameral bimatoprost implants. Methods: We retrospectively reviewed the records of 46 eyes from 38 patients who received an intracameral implant containing 10 µg of bimatoprost as a replacement or addition to their existing eyedrop regimen and investigated IOP, eyedrop usage, and adverse effects. Results: Patients were followed for an average of 274 ± 104 (mean ± standard deviation) days after implant. Mean reduction in IOP (mmHg) at 3 months ±30 days, 6 months ±60 days, and 12 months ±90 days postoperation compared to baseline was 1.26 ± 2.53 (P = 0.002), 0.93 ± 4.71 (P = 0.098), and 1.35 ± 5.24 (P = 0.053), respectively. Reduction in eyedrops at 3 months ±30 days, 6 months ±60 days, and 12 months ±90 days postoperation compared to baseline were 0.62 ± 0.49 (P < 0.001), 0.55 ± 0.73 (P < 0.001), and 0.51 ± 0.71 (P < 0.001), respectively. Fifteen eyes (32.6%) experienced implant failure, defined as either restarting IOP-lowering eyedrops or undergoing surgical intervention, at an average of 260 ± 122 days after implant. Conclusions: While some patients eventually experienced implant failure, intracameral bimatoprost implants may result in fewer adverse reactions and successfully lower IOP and eyedrop burden over a longer period than previously reported.


Assuntos
Pressão Intraocular , Hipertensão Ocular , Humanos , Bimatoprost/farmacologia , Soluções Oftálmicas , Estudos Retrospectivos , Anti-Hipertensivos/farmacologia , Amidas , Cloprostenol/efeitos adversos , Hipertensão Ocular/tratamento farmacológico
20.
Curr Oncol ; 30(4): 3609-3626, 2023 03 25.
Artigo em Inglês | MEDLINE | ID: mdl-37185388

RESUMO

Millions of new cancer patients receive chemotherapy each year. In addition to killing cancer cells, chemotherapy is likely to damage rapidly proliferating healthy cells, including the hair follicle keratinocytes. Chemotherapy causes substantial thinning or loss of hair, termed chemotherapy-induced alopecia (CIA), in approximately 65% of patients. CIA is often ranked as one of the most distressing adverse effects of chemotherapy, but interventional options have been limited. To date, only scalp cooling has been cleared by the US Food and Drug Administration (FDA) to prevent CIA. However, several factors, including the high costs not always covered by insurance, preclude its broader use. Here we review the current options for CIA prevention and treatment and discuss new approaches being tested. CIA interventions include scalp cooling systems (both non-portable and portable) and topical agents to prevent hair loss, versus topical and oral minoxidil, photobiomodulation therapy (PBMT), and platelet-rich plasma (PRP) injections, among others, to stimulate hair regrowth after hair loss. Evidence-based studies are needed to develop and validate methods to prevent hair loss and/or accelerate hair regrowth in cancer patients receiving chemotherapy, which could significantly improve cancer patients' quality of life and may help improve compliance and consequently the outcome of cancer treatment.


Assuntos
Antineoplásicos , Neoplasias , Estados Unidos , Humanos , Qualidade de Vida , Alopecia/induzido quimicamente , Alopecia/prevenção & controle , Alopecia/tratamento farmacológico , Crioterapia , Neoplasias/tratamento farmacológico , Antineoplásicos/efeitos adversos
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