Tazarotene Gel Research Articles

Binary Ethosomal Gel for Enhanced Transdermal Delivery of Tazarotene: Development, Refinement, in vitro Evaluation, and Skin Penetration Investigations

Background: Tazarotene (TZ) is a novel acetylenic class retinoid that selectively targets RARβ/γ. It is not particularly soluble or bioavailable, yet it is used to treat melanoma. Objective: To improve the tazarotene gel formula's transdermal distribution. Methods: TZ-incorporated binary ethosomes (TZ-BES) were developed for the current study. The cold technique and optimized Box-Behnken statistical design tools were used to synthesize the TZ-BES. The improved ethosome (TZ-BES13) was mixed with carbopol gel and tested for stability and ex vivo skin penetration, as well as viscosity, pH, spreadability, and drug content. Results: The optimal ethosomes (TZ-BES13) had a vesicle size of 168 nm, a PDI of 0.367, a zeta potential of -30 mV, and an entrapment effectiveness of 79.94%. TZ is enclosed in the ethosome matrix, as seen by the differential scanning calorimetry thermogram. FTIR shows that the TZ and additives are compatible. TZ-BES13-G2, the optimized TZ-BES13 gel, has a spreadability of 7.82 cm2, a pH of 6.52, a viscosity of 17235, and a drug content of 99.82±1.04%. Compared to the plan TZ-gel (43.54%), the TZ-BES13-G2 exhibits a much higher TZ release (89.22%). In 6 hours, rat abdomen skin permeability for TZ-BES13-G2 was 66.22±3.31%, much greater than that of plan TZ-gel (24.67%). The flow of TZ-BES13-G2 was 2.68 times greater than that of plan TZ-gel. The stability analysis showed that the formulation's properties had not changed significantly. Conclusion: Ethosomal gel offers an alternative mode of TZ administration when used topically.

Safety of Tazarotene 0.045% Lotion and Hyperpigmentation Improvements in Black Participants With Moderate-to-Severe Acne

Introduction: Post-inflammatory hyperpigmentation (PIH) that results from acne in patients with skin of color may be more distressing than the acne itself, and likely impacts patients with higher skin phototypes more greatly than those with lower skin phototypes. Topical retinoids, a mainstay of acne treatment, can also reduce hyperpigmentation. For example, significant PIH improvements with a cream formulation of the retinoid tazarotene (0.1%) were observed following 16 weeks of treatment in patients with acne. However, skin irritation and other skin reactions may limit use of some tazarotene gel and cream formulations. A hydrating, lower-dose tazarotene 0.045% lotion formulation utilizes polymeric emulsion technology to allow for more efficient delivery of tazarotene into dermal layers while reducing potential for skin irritation. This pooled, post hoc analysis evaluates safety of tazarotene 0.045% lotion and its effect on hyperpigmentation in Black individuals with acne.
 Methods: In two identical phase 3 randomized, double-blind, vehicle-controlled, studies (NCT03168321; NCT03168334), participants aged ≥9 years with moderate-to-severe acne (Evaluator's Global Severity Score of 3/4) were randomized (1:1) to once-daily tazarotene 0.045% or vehicle lotion for 12 weeks. Safety evaluations included adverse events (AEs) reports and investigator-assessed hyperpigmentation (4-point scale: 0 [none] to 3 [severe]). Post hoc analyses were based on participants’ self-identification of race, including ‘Black or African American’ (herein referred to as Black).
 Results: Of 1,614 participants randomized in the two phase 3 studies, 262 (16%) self-identified as Black. The safety population comprised 253 Black participants. The most common TEAEs with tazarotene 0.045% lotion were at the application site: pain (6.6%), exfoliation (5.0%), and dryness (3.3%). No Black participants reported application site irritation or dermatitis with tazarotene lotion. Hyperpigmentation rates in Black participants, which were high at baseline, decreased by week 12 with tazarotene treatment (40.5% to 31.4%) compared to vehicle (37.9% to 37.2%).
 Conclusions: Acne regimens that maximize efficacy while mitigating irritation is key to managing acne in patients with skin of color, given the higher pigmentary alteration risk in melanin-rich skin. Tazarotene 0.045% lotion was safe and well tolerated in Black participants, with no application-site irritation or dermatitis after 12 weeks of once-daily treatment. Tazarotene also led to improvements in hyperpigmentation, an inflammation-associated sequala of acne. As PIH can take longer than 12 weeks to resolve with treatment, additional improvements in hyperpigmentation may be expected with continued tazarotene 0.045% lotion use.
 Support: Ortho Dermatologics.

A comparative study of Ozonized olive oil versus Tazarotene gel in the Treatment of Onychomycosis

A comparative study of Ozonized olive oil versus Tazarotene gel in the Treatment of Onychomycosis

The comparative study to determine the efficacy of 0.05% tazarotene gel versus 0.1% adapalene gel in patients of facial acne vulgaris

Introduction: Acne vulgaris is one of the most common skin disorders that present to Dermatology clinics. The majority of the patients suffer from mild-to-moderate acne, for which topical retinoids form the mainstay of treatment. Aims and Objectives: The aim of this article is to study and determine the efficacy and tolerability of 0.05% tazarotene gel against 0.1% adapalene gel in facial acne vulgaris. Materials and Methods: Eighty-two facial acne vulgaris patients were randomly divided into two groups. Group A was given 0.05% tazarotene gel, and group B received 0.1% adapalene gel to be applied overnight for a period of 8 weeks. Lesion counting and photographs were recorded every 15 days. Results: The mean difference on first follow-up from baseline for tazarotene and adapalene was 6.80 ± 6.42 and 1.48 ± 10.44, and the P-value was 0.013. The final follow-up visit values were 34.77 ± 23.73 and 25.48 ± 13.04, with a P-value of 0.051. The mean percentage change from baseline to last follow-up for tazarotene and adapalene was 60% and 51%, respectively, which were statistically significant for both groups (P < 0.05). More patients in the tazarotene group developed cutaneous side effects such as erythema and burning sensation than those in the adapalene group (P < 0.05). conclusion: About 0.05% tazarotene gel has better efficacy than 0.1% adapalene, though associated with more side effects. It can be used as a topical adjunct or as monotherapy in mild-to-moderate facial acne vulgaris.

Fabric phase sorptive extraction combined with high-performance liquid chromatography-photodiode array detection for the determination of tazarotene in gel dosage forms

Tazarotene, a member of the acetylenic class of retinoids, is a third-generation prescription topical retinoid sold as a cream, gel, or foam. In its gel or cream formulations, tazarotene is at a concentration of either 0.1 % or 0.05 %. Fabric phase sorptive extraction membranes are used to selectively isolate and preconcentrate target analytes from different sample matrices. In this study, the tazarotene gel formulation was directly applied to fabric phase sorptive extraction membranes and extracted through a mixture of acetonitrile and water (80:20, v/v) to obtain a clean product free of colloidal suspension of tazarotene gel formulation. The final solutions were injected into an HPLC system equipped with a Zorbax 5 μm Phenyl-Hexyl LC Column (250 × 4.6 mm). Injection volume was 50 μL and UV detection was performed at 326 nm. The flow rate was 1.0 mL min−1 while using an isocratic elution with a mixture of ammonium acetate (50 mM) and methanol (15:85, v/v) as the mobile phase. The method was validated according to ICH guideline Q2 (R1) and successfully applied to gel formulations including 0.01 % tazarotene. This is the first reported application of fabric phase sorptive extraction in the analyses of gel formulations. The capability of fabric phase sorptive extraction membranes to clean up the sample matrix and prepare active pharmaceutical ingredients to be analyzed with acceptable recovery (>98.0 %) and reproducibility may encourage quality control laboratories to use fabric phase sorptive extraction in routine applications.

Tazarotene gel promotes healing of deep tissue injury in mice

ABSTRACT We investigated the efficacy and molecular mechanisms of tazarotene gel for healing deep tissue injury (DTI). We used male C57BL/6J mice to establish a DTI model. Animals were divided randomly into control, tazarotene gel and purilon gel groups. We injected 100 ul tazarotene gel, purilon gel or saline every 48 h for 20 days. Hematoxylin and eosin staining was used to observe pathological changes on days 14 and 21. The mRNA and protein expression of VEGF-α, TGF-β1 and HIF-1α were detected by qRT-PCR and western blot, respectively. Wound sites exhibited accelerated healing by 20 days in the tazarotene gel group. Fewer inflammatory cells and more granulation tissue were found in both experimental groups compared to controls. The mRNA and protein expression of VEGF-α and TGF-β1 in the experimental groups were increased compared to the control group by day 14. Expression of HIF-1α in the experimental groups was significantly less than in the controls. Tazarotene gel promoted wound healing independent of the HIF-1α/VEGF signalling pathway during tissue repair of DTI. Tazarotene and purilon gels exhibited similar macroscopic healing of wounds and expression of genes and proteins.

Topical Imiquimod for Lentigo Maligna: Survival Analysis of 103 Cases With 17 Years Follow-up.

Topical imiquimod 5% cream has been investigated as off-label primary or adjuvant treatment for melanoma in situ, lentigo maligna type (LM). Herein, we present the largest known case series of lentigo maligna treated with topical imiquimod, with up to 17 years of follow-up, and include a recurrence-free survival analysis. In this case series, 103 lesions were retrospectively evaluated for treatment response and recurrence following a course of topical imiquimod with or without tazarotene gel 0.1% pretreatment between January 1, 2002 and March 31, 2019, and prospectively followed through November 15, 2019. Over median follow-up of 5.1 years (mean = 6.2 years, S = 5.2 years, range, 0.08&ndash;17.1 years), including 29.1% LM with &gt;10 years follow-up, we observed a response rate of 97.1% (100/103), with 8 local recurrences (8/100, 8.0%) developing at mean 2.9 years (SD: 2.7 years). Local recurrence was significantly associated with a history of failed excision (P= 0.001), &lt;60 applications of imiquimod (P= 0.04) and partial clinical clearance (P= 0.0003). Recurrence-free survival analysis demonstrated significant risk-stratification for low and high-risk groups (P= 0.0001). Long term risk for recurrence showed significant differences among low- and high-risk cases, with low-risk cases demonstrating favorable long-term outcomes, comparable to conventional and staged surgery. Our observed low recurrence in a large case series with long-term follow-up suggests the efficacy of topical 5% imiquimod for LM and emphasizes the need for randomized control trials comparing imiquimod with, or as an adjunct to, surgical treatment. J Drugs Dermatol. 2021;20(3):346-348. doi:10.36849/JDD.5660.

Fixed combination of tazarotene and betamethasone dipropionate for treatment of psoriasis vulgaris: The result of a phase 3, multicenter, randomized controlled trial.

Long-term use of corticosteroids or local use of tazarotene (TAZ) alone for the treatment of psoriasis cause safety issues and low compliance rates. Combining these two may optimize their efficacy and minimize safety concerns. This study aimed to evaluate the clinical efficacy and safety of a fixed combination of TAZ 0.05% and betamethasone dipropionate 0.05% (BM) for psoriasis vulgaris. A multicenter, randomized, single-blinded, controlled phase 3 clinical trial was conducted. A total of 600 Chinese subjects with psoriasis vulgaris were randomized (3:1:1) to TAZ/BM cream, TAZ gel or BM cream groups for 6weeks with an 8-week follow up. The primary efficacy assessment end-point was 75% improvement in Psoriasis Area and Severity Index (PASI-75) at 6weeks. Secondary outcome assessments included PASI-90, percentage of PASI decrease and so forth. Safety and treatment-related adverse events were monitored throughout the study. Our results demonstrated that the TAZ/BM group exhibited statistically significant superiority in PASI-75 over TAZ (6.74% vs 1.67%) within 2weeks. After 6weeks of treatment, PASI-75 was 44.94% in the TAZ/BM group while 19.17% and 35.00% in the TAZ and BM group, respectively. At the 8-week follow up, the relapse rate of the TAZ/BM group was significantly lower than the BM group (10.62% vs 29.63%, P=0.0269) though comparable with the TAZ group (10.00%). The most frequently reported treatment-related adverse event was mild to moderate level of skin irritation events. TAZ/BM combination has significant advantages over TAZ, including satisfying efficacy, rapid onset and reduced local stimulation. Meanwhile, compared with BM, it has the advantages of longer relief time and reduced clinical relapse rate. The TAZ/BM combination drug provides psoriatic patients an alternative drug with high efficacy and low relapse rate and safety concerns.

Effect of Dapsone Gel 7.5% Compared to Tazarotene Gel 0.1% for Treatment of Acne Vulgaris

Effect of Dapsone Gel 7.5% Compared to Tazarotene Gel 0.1% for Treatment of Acne Vulgaris

DEVELOPMENT AND OPTIMIZATION OF TAZAROTENE LOADED SOLID LIPID NANOPARTICLES FOR TOPICAL DELIVERY

Objective: Psoriasis is an unswervingly recurring, inflammatory, autoimmune disorder of the skin, disturbing about 2–5% of the world population. The main objective for this investigation is to develop and optimize the solid lipid nanoparticles (SLN) formulation of tazarotene for effective drug delivery.&#x0D; Methods: Tazarotene SLNs were fabricated by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency (EE). In view of the outcomes from the examinations of the responses acquired from Taguchi design, three diverse independent variables including sonication time (s), lipid to drug ratio (w/w), and surfactant concentration (%) were carefully chosen for further investigation utilizing central composite design. The lipid dynasan-116, surfactant poloxamer-188, and cosurfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, drug EE, zeta potential, in vitro drug release, and stability.&#x0D; Results: The prepared nanoformulations were evaluated for different parameters and found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F1) was found to be 98.12±1.52%, whereas pure drug release was 42.12 after 60 min, and the major mechanism of drug release follows zero-order kinetics release data for optimized formulation (F1) with non-Fickian (anomalous) with a strong correlation coefficient (R2=0.98598) of Korsmeyer-Peppas model. Transmission electron microscopy analysis has demonstrated the presence of individual nanoparticles in spherical shape, and the results were also compatible with particle size measurements. The drug content of tazarotene gel formulation was found to 98.96±0.021%, and the viscosity of gel formulation at 5 rpm was found to be 5.98×103±0.34×103 cp. The release rate (flux) of tazarotene across the membrane and expunged skin diverges pointedly, which specifies the barrier nature of skin. The flux value for SLN based gel formulation (193.454±4.324 μg/cm2/h) was found to be higher than that for marketed gel (116.345±2.238 μg/cm2/h). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin.&#x0D; Conclusion: From the obtained results, the topically oriented SLN-based gel formulation of tazarotene could be useful in providing effective and site-specific psoriasis treatment.

Effect of dapsone gel 7.5% compared to tazarotene gel 0.1% for treatment of acne vulgaris

Effect of dapsone gel 7.5% compared to tazarotene gel 0.1% for treatment of acne vulgaris

Development of a simple method for simultaneous determination of tazarotene and betamethasone dipropionate and their metabolites using LC-MS method and its application to dermatopharmacokinetic study.

In our study, a method for the determination for tazarotene and betamethasone dipropionate in human tissue-engineered skin was established. Tazarotene gel, betamethasone dipropionate cream or a combination cream was administered to the skin. Then the skin was taken off at 0.25, 0.75, 1.75, 3, 5, 8, 12, 24, 36, 48 h time points after the residual drug was removed. The concentrations of tazarotene, betamethasone dipropionate and their major metabolites in skin were determined by LC-MS. Tazarotene and tazarotenic acid were detected in the concentration range of 2-200 μg/mL with an LLOQ of 2 μg/mL. Betamethasone dipropionate was detected in the concentration range 0.5-300 μg/mL with an LLOQ of 0.5 μg/mL, and betamethasone was detected at 2-200 μg/mL with an LLOQ of 2 μg/mL. The intra- and inter-day precisions of the four analytes in the skin homogenate were all <15% (RSD, %). The results showed that tazarotene could be metabolized to tazarotenic acid and betamethasone dipropionate could be metabolized to betamethasone in tissue-engineered skin. The results also revealed that this method was suitable for the simultaneous determination of tazarotene, betamethasone dipropionate and their metabolites in tissue-engineered skin.

Efficacy of photodynamic therapy combined with topical interventions for the treatment of actinic keratosis: a meta-analysis.

Photodynamic therapy (PDT) is a highly effective treatment option for patients with actinic keratoses (AK). However, efficacy can be reduced by insufficient illumination or hyperkeratotic nature of lesions. To investigate if PDT combined with a topical intervention is superior to monotherapy in terms of efficacy and tolerability. A systematic literature research was conducted in Medline, Embase and CENTRAL. Pertinent trial registers were hand-searched for eligible randomized controlled trials (RCTs) until 20 August 2018. Results were pooled using a random effects model to calculate relative risks (RR) or mean differences. The risk of bias was assessed with the Cochrane Risk of Bias Tool. The quality of evidence was estimated for each outcome of interest according to GRADE. Out of 1800 references initially identified, 10 RCTs with a total sample size of n=277 were included. Four studies investigated a combination of PDT with imiquimod cream, three with 5-fluorouracil cream and one each with ingenol mebutate gel, tazarotene gel and calcipotriol ointment, respectively. Patients treated with a combination showed higher participant complete (RR 1.63; 95% CI 1.15-2.33; P=0.007) and partial clearance rates (RR 1.19; 95% CI 0.84-1.67; P=0.33). Similarly, the lesion-specific clearance was higher for PDT plus topical intervention compared to monotherapy (RR 1.48; 95% CI 1.04-2.11; P=0.03). A subgroup analysis was performed for PDT combined with imiquimod, revealing an increased participant complete clearance rate compared to monotherapy (RR 1.57, 95% CI 1.09-2.25, P=0.02). PDT-induced pain and local skin reactions after treatment were poorly reported. The studies were estimated at high risk for performance and detection bias. The combination of PDT with another topical drug intervention does improve AK clearance rates compared to either monotherapy alone. This study highlights that the sequential application of two field-directed treatments represents an efficient approach in patients with multiple AK and field cancerization.

Topical Tazarotene Gel, 0.1%, as a Novel Treatment Approach for Atrophic Postacne Scars: A Randomized Active-Controlled Clinical Trial.

Evidence is robust for the effectiveness of microneedle therapy in the management of postacne atrophic scarring. A home-based topical treatment with an efficacy comparable to microneedling would be a useful addition in the armamentarium of acne scar management. To compare the efficacy of topical tazarotene gel, 0.1%, with microneedling therapy in the management of moderate to severe atrophic acne scars. Prospective, observer-blinded, active-controlled, randomized clinical trial with 6 months of follow-up conducted between June 2, 2017, and February 28, 2018, at a tertiary care hospital in India. Thirty-six patients with grade 2 to 4 facial atrophic postacne scars and without a history of procedural treatment of acne scars within the previous year were recruited. Analyses were conducted using data from the evaluable population. Both halves of each participant's face were randomized to receive either microneedling or topical tazarotene therapy. Microneedling was conducted on 1 side of the face with a dermaroller having a needle length of 1.5 mm for a total of 4 sessions during the course of 3 months. Participants were instructed to apply topical tazarotene gel, 0.1%, to the other side of the face once every night during this same period. Patients were followed up at 3 and 6 months by a blinded observer, and improvements in acne scar severity based on Goodman and Baron quantitative and qualitative scores and a subjective independent dermatologist score (range, 0-10, with higher scores indicating better improvement) were assessed. Patient satisfaction was assessed using a patient global assessment score (ranging from 0 for no response to 10 for maximum improvement) at these follow-up visits. There were 36 participants (13 men and 23 women; mean [range] age, 23.4 [18-30] years), and the median (interquartile range [IQR]) duration of acne was 6 (4-8) years. For the 34 participants included in the complete data analyses, the median (IQR) quantitative score for acne scar severity at the 6-month follow-up visit following treatment with either tazarotene (from a baseline of 8.0 [6.0-9.8] to 5.0 [3.0-6.0]) or microneedling (from a baseline of 7.0 [6.0-10.8] to 4.5 [3.0-6.0]) indicated significant improvement (P < .001) that was comparable for both treatments (median [IQR] change in severity score from baseline, 2.5 [2.0-4.0] vs 3.0 [2.0-4.0]; P = .42). By contrast, median qualitative acne scar scores were the same for both treatment groups at baseline and did not significantly change following either treatment. The present clinical trial showed comparable outcomes of both treatments for the overall improvement of quantitative facial acne scar severity. 1. ClinicalTrials.gov identifier: NCT03170596.

Porokeratotic Eccrine Ostial and Dermal Duct Nevus and Porokeratotic Eccrine and Hair Follicle Nevus: Is Nomenclature "Porokeratotic Adnexal Ostial Nevus" More Appropriate?

Porokeratotic Eccrine Ostial and Dermal Duct Nevus and Porokeratotic Eccrine and Hair Follicle Nevus: Is Nomenclature "Porokeratotic Adnexal Ostial Nevus" More Appropriate?

Real-time simultaneous detection of microbial contamination and determination of an ultra low-content active pharmaceutical ingredient in tazarotene gel by near-infrared spectroscopy.

This paper proposes and proves a real-time and non-destructive strategy for sensitive and simultaneous detection of microbial contamination and determination of an ultra low-content active pharmaceutical ingredient in tazarotene gel by near-infrared (NIR) spectroscopy. In this experiment, 88 samples of tazarotene gel (0.41–0.65 mg g−1 of tazarotene) were prepared using the standard addition method. Among them, 47 samples were inoculated with 50 μl of different concentrations of Escherichia coli (E. coli) DH5a in Luria–Bertani (LB) broth to give 1–4 log CFU g−1 of E. coli DH5a in the gel, 6 samples with 50 μl of LB broth, and 35 samples with nothing. Based on the gel NIR transflectance spectra, E. coli DH5a in the gel was detected by the counter propagation artificial neural network (CP-ANN) model with a classification accuracy of 100.0%, while tazarotene in the gel was simultaneously determined by the partial least squares regression (PLS) model with a root mean square error of cross-validation of 0.0232 mg g−1. Furthermore, 9 samples of real tazarotene gel were used to verify the practicality of the established NIR spectroscopy. The developed NIR strategy can be used to correctly and quickly release the pharmaceutical gels, required for sensitive and simultaneous control of microbial contamination and the active pharmaceutical ingredient (API) content, to the next stage.

Tazarotene gel with narrow-band UVB phototherapy: a synergistic combination in psoriasis

Background: Narrow-band UVB (NB-UVB) has been shown to be one of the most effective treatment modalities for psoriasis. Tazarotene, a known effective anti-psoriatic modality, when combined with NB-UVB may enhance the therapeutic success.Objective: To study clinical efficacy and safety of combination of NB-UVB with topical tazarotene 0.05% gel in psoriasis.Method: Thirty patients with plaque psoriasis having symmetrical lesions were enrolled for 12 weeks. All patients were instructed to apply tazarotene gel on target plaque on left side of body once daily. In addition, the whole body was irradiated with NB-UVB twice weekly. Efficacy was assessed by target plaque scoring and number of treatment sessions for clearance.Result: Our study resulted in 3 key findings: Firstly, therapeutic efficacy of NB-UVB was enhanced by addition of tazarotene. This enhanced efficacy was more apparent in decreasing scaling and thickness as compared to decrease in erythema. Secondly, combination therapy showed faster clearance of target plaques, with reduction in mean number of treatment sessions. Thirdly, mean cumulative NB-UVB dose needed to achieve clearance of target plaques was significantly reduced with combination therapy.Study limitations: The study was not randomized or controlled, but an open-label trial. The study period was relatively short, i.e., 12 weeks, without any follow-up period.Conclusion: Tazarotene gel significantly enhances the therapeutic efficacy of NB-UVB irradiation with faster clearance and without serious side effects.

Simultaneous determination of tazarotene and its active metabolite tazarotenic acid in minipig plasma by LC-MS/MS and its application in pharmacokinetic study after topical administration of tazarotene gel.

To study the systemic exposure of tazarotene formulation after topical administration, a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of tazarotene and tazarotenic acid in minipig plasma. Similar extraction recoveries for both analytes were obtained after the plasma samples were acidified by glacial acetic acid (5%) and extracted by ethyl ether-cyclohexane (4:1, v/v). Separation of the analytes was achieved within a short time by the addition of 0.1% formic acid to the mobile phase. Gradient elution was used to avoid the matrix effect. The method was linear over the concentration range of 10-600 pg/mL for both analytes. The data of intra- and inter-run precision and accuracy were lower than 5.2%, 7.3% and 7.3% for both analytes. The developed method can be applied to investigate the transdermal pharmacokinetics and the systemic exposure of tazarotene formulation after topical administration.

Evaluation of change in the skin concentration of tazarotene and betamethasone dipropionate based on drug–drug interaction for transdermal drug delivery in miniature pig

1. The present study was designed to investigate drug–drug interaction in a new combination cream which contains both tazarotene (TZRT) and betamethasone dipropionate (BTMSDP) by comparing the pharmacokinetic (PK) behaviors of TZRT, BTMSDP, and their major metabolites, tazarotenic acid (TZRTAC) and betamethasone (BTMS) with those in the commonly prescribed TZRT gel and BTMSDP cream.2. The trial was performed on six Bama mini-pigs. The different regions on the back side of each pig were randomly assigned to one of three treatment groups: TZRT 0.05% gel, BTMSDP 0.05% cream, and combination cream. The stratum corneum and epidermis–dermis samples were collected at various times after drug administration and analyzed for TZRT, TZRTAC, BTMSDP, and BTMS by LC-MS/MS. Compared with TZRT gel alone, TZRT + BTMSDP did not significantly change the PK profiles of TZRT; neither did BTMSDP + TZRT significantly change the PK profiles of BTMSDP, compared with the BTMSDP cream alone. In addition, the concentrations of TZRTAC and BTMS in most samples were below the lower limit of quantitation (LLOQ).3. The results suggest that there was no significant drug–drug interaction trend between TZRT and BTMSDP in the process of transdermal permeation of combination cream into the stratum corneum and epidermis–dermis of mini-pigs.

Tazarotene-induced gene 3 may affect inflammatory angiogenesis in psoriasis by downregulating placental growth factor expression.

Tazarotene-induced gene 3 may affect inflammatory angiogenesis in psoriasis by downregulating placental growth factor expression.