Topical Acne Therapy Research Articles

Efficacy of topical treatments for mild‐to‐moderate acne: A systematic review and meta‐analysis of randomized control trials

AbstractAcne is a common skin condition, but little data exist on the comparative efficacy of topical acne therapies. We conducted a systematic review and network meta‐analysis to evaluate the efficacy of topical therapies for mild‐to‐moderate acne. Searches in PubMed/MEDLINE, Cochrane CENTRAL via Ovid, Embase via Ovid and Web of Science were conducted on 29 November 2021. Randomized controlled trials examining ≥12 weeks of topical treatments for acne vulgaris in subjects aged 12 and older were included. Main outcomes were absolute or percent change in acne lesion count and treatment success on the Investigator's Global Assessment scale. Thirty‐five randomized clinical trials with 33,472 participants comparing nine different topical agents were included. Adapalene‐benzoyl peroxide (BPO), clindamycin‐BPO and clindamycin‐tretinoin demonstrated the greatest reduction in non‐inflammatory (ratio of means [RoM] 1.76; 95% CI [1.46; 2.12], RoM 1.70; 95% CI [1.44; 2.02] and RoM 1.87; 95% CI [1.53; 2.30], respectively), inflammatory (RoM 1.56; 95% CI [1.44; 1.70], RoM 1.49; 95% CI [1.39; 1.60] and RoM 1.48; 95% CI [1.36; 1.61], respectively) and total lesion count (ROM 1.67; 95% CI [1.47; 1.90], RoM 1.59; 95% CI [1.42; 1.79] and RoM 1.64; 95% CI [1.42; 1.89], respectively) compared to placebo. All single agents outperformed placebo except tazarotene, which did not significantly outperform placebo for inflammatory and non‐inflammatory lesion count reduction. Most combination agents significantly outperformed their individual components in lesion count reduction and global assessment scores, except for clindamycin‐tretinoin and clindamycin‐BPO, which did not significantly outperform tretinoin (RoM 1.13; 95% CI [0.94; 1.36]) and BPO (RoM = 1.15, 95% CI [0.98; 1.36]), respectively, for non‐inflammatory lesion reduction. There was no significant difference amongst most single agents when evaluating lesion count reduction. Combination agents are generally most effective for mild‐to‐moderate acne; however for non‐inflammatory acne, the addition of clindamycin in topical regimens is unnecessary and should be avoided.

Formulasi gel ekstrak daun sirih cina (Peperomia pellucida L. Kunth) variasi carbopol 940 serta uji fisik dan stabilitasnya

Chinese betel leaf (Peperomia pellucida L. Kunth) contains tannins, alkaloids, saponins and flavonoids which can inhibit the growth of Propionibacterium acnes bacteria. Gel preparations are suitable for topical therapy of acne. The gelling agent used was carbopol 940. The purpose of this study was to determine the effect and concentration of carbopol 940 which produced the best physical properties of Chinese betel leaf extract gel preparations. This research is an experimental research. Gel preparations were made with various concentrations of carbopol 940 0.5%, 1.0%, 1.5%, and 2.0% then organoleptic examination, homogeneity, pH, adhesion, spreadability, viscosity, skin irritation, physical stability , and hedonic. The data obtained were analyzed with SPSS (trial) using the One Way ANOVA method. The results showed that variations in carbopol 940 concentrations had an effect on organoleptic, adhesiveness, pH, spreadability, viscosity, and hedonics but had no effect on homogeneity, physical stability, and skin irritation. Carbopol 940 concentration of 1.0% produced the best preparation compared to concentrations of 0.5%, 1.5% and 2.0% in terms of physical properties and statistical analysis.

P102 Severe atopic eczema is associated with reduced acne vulgaris in Bangladeshi children and young adults: a retrospective analysis from a cross-sectional study

Abstract Atopic eczema (AE) is the most common inflammatory dermatosis, affecting up to 20% of children. Loss of function (LoF) mutations in FLG are the most strongly implicated genetic risk factor for eczema. To understand the effect of FLG on the pathobiology of AE, we knocked down FLG in primary keratinocytes using short hairpin RNA and performed phosphoproteomic analysis, which showed downregulation of the AKT signalling pathway, confirmed using Western blotting to phospho-AKT and immunostaining of biopsies from patients with AE. Given that AKT signalling is increased in acne vulgaris, we hypothesized that loss of FLG may protect patients with AE from acne. The Tower Hamlets Eczema Assessment (THEA) study is a cross-sectional study that aims to phenotype and genotype 1000 Bangladeshi children and young adults with AE. So far, 620 participants have undergone genotyping, 37% of whom have LoF mutations in FLG. We selected patients from this cohort who were older than 12 years of age. In total, 204 patients (99 FLG wild type, 86 heterozygotes, 19 compound heterozygotes) were included. We identified a diagnosis of acne or previous prescription of topical acne therapies or tetracycline antibiotics from the patients’ general practice e-health records. We stratified the patients by genotype, Eczema Area and Severity Index (EASI) score, Patient Oriented Eczema Measure (POEM) score, transepidermal water loss (TEWL) and palmar hyperlinearity groups. The χ2-test was used to determine differences between groups. A lower proportion of patients with AE with FLG mutations had acne (27% wild type vs. 19% FLG mutations), which was more pronounced, but not statistically significant, in the compound heterozygote group (16%). We saw a nonsignificant reduction in acne in patients who had the top 25% of TEWL measurements, those with the most severe form of hyperlinearity and those with higher POEM scores. Patients with severe AE, measured as an EASI score > 21, had a more reduced incidence of acne than those with lower EASI scores (9% vs. 26%; P = 0.04). Overall, this suggests that patients with more severe AE are protected from developing acne. There was insufficient evidence to establish if this was mediated by a reduction in filaggrin (FLG) and AKT signalling. This may be because the groups were too small to determine this. Given that all patients with severe AE have reduced FLG expression regardless of genotype, it is possible that this is mediated through FLG–AKT signalling.

Ethosomes Loaded with Spiranolactone for Acne treatment through Topical Gel Formulation

The goal of this work was to create Spiranolactone-loaded ethosomes and use them as a topical acne therapy gel. The size of the vesicle, Spiranolactone filling, and encapsulation function of ethosomes were all created and tested. Improved ethosomes were produced as Carbomer 974 gels and tested for transdermal permeability and porosity, as well as in vitro transplantation, against traditional hydroethanolic gels. With Spiranolactone efficiency of loading and encapsulation of 0.433±0.006 mg/mL and 39.29±0.65 percent, the produced ethosomes had a mean size of vesicle 68.1±1.8 nm. A well-developed ethosomal gel had 2.5 times the transdermal flux and 2.1 times the skin implantation of regular gels. For mild skin irritation, ethosomal gel has a superior anti-acne impact. This research reveals that ethosomal formation is a good way to transfer spiranolactone to the skin, and that spiranolactone ethosomal gels could be used to treat acne in the future.

Detailed overview on pharmaceutical dosage forms in treatment of acne

Acne vulgaris is a skin condition characterized by an obstruction or inflammation of the oil glands, present on skin's surface, which are collectively termed as pilosebaceous units. The skin on face, back, and upper chest have a greater number of sebaceous follicles. Topical, systemic, or combination therapy can be used to treat acne, while mild and moderate acne are generally treated with topical therapy. Topical acne therapy has direct access to the target site (skin) prior to reaching the blood stream, thereby reducing the systemic adverse effects of delivery of drug via parenteral or oral routes. Oral antibiotics, on the other hand, are a crucial treatment for acne which have not improved with topical treatment and for inflammatory lesions, such as pustules, nodules, and papules. Due to their capability to improve dermal therapeutics by boosting therapeutic efficacy and lowering adverse effects, nanodelivery technologies, developed to address skin delivery difficulties, have been extensively investigated. The goal of this study is to go through the many types of pharmacological dosage forms that are available for the treatment of acne.

Fibrous palygorskite clays as versatile nanocarriers for skin delivery of tea tree oils in efficient acne therapy

This paper presents a facile approach to develop palygorskite (Pal), a fibrous clay mineral, as a delivery system of tea tree oil (TTO) for topical acne therapy. The obtained TTO-Pal composite showed an efficient loading of TTO (27.4%) with a selective accumulation of terpine-4-ol and 1,8-cineole (two major antimicrobial TTO constituents), sustained release of TTO at skin physiological conditions (pH5.4, 32 °C) and superior skin sebum (2.2 g/g) absorbability. In vitro toxicological assessments showed that the Pal incorporation strategy significantly reduced the acute contact toxicity of TTO. The antimicrobial results revealed a preferable bacteriostatic effect for the TTO-Pal system towards opportunistic dermal pathogens (Escherichia coli, Staphylococcus aureus and Propionibacterium acnes) over the beneficial bacterium (Staphylococcus epidermis). Moreover, TTO-Pal based formulations exhibited pronounced clinical therapeutic efficacy in treating facial acne by rapidly reducing inflamed lesions, modulating skin sebum overproduction and restoring barrier function. This is the first report of using fibrous clay as a biocompatible nanocarrier system for topical delivery of essential oils in efficient management of facial acne with both in vitro and in vivo evidences, which may open perspectives for fibrous clay-drug delivery system in topical application and expand the high added value development of this mineral resource in the advanced healthcare fields.

New Developments in Topical Acne Therapy.

Acne vulgaris is a common chronic inflammatory disease with a multifactorial pathogenesis. Although myriad acne treatments are available, current options may not be sufficient because of a lack of efficacy, limited tolerability, or burden of cost to patients. In this review, we highlight recently approved topical acne treatments, as well as those currently in clinical trials. Novel formulations of tretinoin, tazarotene, and minocycline provide modifications of and improvements to existing products. Trifarotene, a novel fourth-generation retinoid, has demonstrated improved tolerability compared with existing topical retinoids. Clascoterone is a novel first-in-class antiandrogen that topically addresses the hormonal etiology of acne. The late-phase clinical trials pipeline consists of agents with bactericidal and anti-sebum mechanisms. Although it is evident that acne treatments continue to evolve, it is important to recognize the need for further comparative studies among new and existing agents to define optimal treatment algorithms that address not only safety and efficacy but also cost-effective care.

The prospects of finding new treatments for acne

An important role in the development of acne is played by the activity of the skin microflora (namely the bacteria Propionibacterum acnes) and members of the genus Staphylococcus. In the schemes of complex treatment of patients with this disease, antibiotics from among macrolides or lincosamides are mainly used. It is of interest to study the current state of susceptibility of staphylococci and propionic bacteria to these drugs, as well as to other antimicrobial agents in order to determine the prospects for expanding the arsenal of methods for treating acne. The aim of the study was to study the susceptibility of microorganisms involved in the development of acne to antimicrobials and antagonistic effects of probiotic strains of lactobacilli. We conducted a bacteriological study of the content of rash elements in 60 patients with acne. The biological characteristics of 40 strains of Staphylococcus spp. and 15 strains of Propionibacterum acnes isolated and researched. The sensitivity of microorganisms to antibiotics and antiseptics was determined by the disco-diffusion method and the method of serial double dilutions of drugs in a liquid nutrient medium. Determination of the sensitivity of acne pathogens to the antagonistic effect of lactobacilli was performed by the method of two-layer agar by reducing the number of microorganisms. The results of the study made it possible to establish that the isolated strains of bacteria show a low level of sensitivity to antimicrobials, which in medical practice are most often used for topical therapy of acne. Only 17.5 % of isolated staphylococcal strains were sensitive to erythromycin, only 45.0 % of strains of this species were sensitive to clindamycin. Strains of Propionibacterum acnes showed a higher level of sensitivity to antibiotics than staphylococci. However, the established indicators do not allow to consider highly effective means for treatment of acne on their basis. At the same time, a high level of sensitivity of acne pathogens to antiseptic drugs decamethoxine and Aeroplysinin 1 and antagonistic effect of Lactobacillus acidophilus was established. Thus, the strains of Propionibacterum acnes and Staphylococcus spp., involved in the development of acne, are characterized by high levels of resistance to erythromycin, clindamycin, chloramphenicol, benzoyl peroxide, which are now the basis of the arsenal of topical therapy for patients with this disease. There is a need to find new effective drugs for the etiotropic therapy of acne.

Hydrogel composite containing azelaic acid and tea tree essential oil as a therapeutic strategy for Propionibacterium and testosterone-induced acne

Azelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (−1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris.Graphical abstract

A pilot study evaluating the efficacy and safety of retinaldehyde-loaded niosomes against mild-to-moderate acne.

Retinoids are the mainstay of topical therapy for acne. To improve the efficacy and minimize the side effects of retinoids, various novel drug delivery mechanisms, including nanoparticles, have been developed. To evaluate the efficacy and safety of a retinaldehyde-loaded niosome (RA-N) nanoemulsion against sebum secretion and keratinization on mild-to-moderate acne. Twenty-three participants exhibiting mild-to-moderate acne with both closed and open comedones were included. They applied a 0.05% RA-N nanoemulsion daily for 4weeks, did not to use any other emollient or topical pharmaceutical, and were asked to report any symptoms and treatment satisfaction. The participants demonstrated significantly fewer closed and open comedones after 2 and 4weeks of treatment than at baseline (*p<0.05). The mean sebum secretion, measured using Sebumeter®, was 327.95±90.20μgcm-2 at baseline and reduced to 282.60±99.70 and 250.65±97.6μgcm-2 , respectively, after 2 and 4weeks of treatment (*p<0.05). The mean desquamation index, determined using Visioscan®, was 10.99±1.69 at baseline and decreased to 9.81±1.10 and 8.89±1.32, respectively, after 2 and 4weeks of treatment (*p<0.05). The application of the RA-N nanoemulsion resulted in a significantly lower desquamation level, suggesting that the RA-N nanoemulsion was well-tolerated without any skin irritation. None of the participants reported a serious adverse event during this study. Our findings suggest that the RA-N nanoemulsion was effective in improving comedones in acne-prone skin and safe for long-term application. Further studies are necessary to investigate the long-term effects of the application of the RA-N nanoemulsion in participants with inflammatory acne and acne scars.

Modern Methods Of Acne And Post-Acne Therapy

In the article, according to the data of foreign scientists and the authors' own observations, modern methods of topical therapy for acne and post-acne are presented.

An overview of adapalene and benzoyl peroxide once-daily topical gel as a therapeutic option for acne

ABSTRACT Introduction Acne vulgaris is the most common skin condition worldwide, and it is associated with substantial psychological comorbidity. Topical therapies – including retinoids, antibiotics, and benzoyl peroxide – are the cornerstones of treatment for patients with acne. The main barriers to care in the treatment of acne are poor adherence to therapy and lack of tolerability. Areas covered Herein, the authors review the safety and efficacy of adapalene/benzoyl peroxide combination gel (0.1%/2.5% and 0.3%/2.5%), as well as its specific mechanisms of action that target acne vulgaris. The authors also offer an expert opinion on the use of adapalene/benzoyl peroxide gel compared with other topical therapies. Expert opinion Adapalene/benzoyl peroxide gel is safe and highly effective in the treatment of acne vulgaris. Its efficacy, tolerability, and ease-of-use are superior to other topical acne therapies, and its use does not contribute to antibiotic resistance. However, the cost of adapalene/benzoyl peroxide gel and lack of available generics may prohibit its use.

NANOEMULSION FOR TOPICAL THERAPY OF ACNE: OPTIMIZATION AND EVALUATION

The present investigation was aimed / carried out to develop a nano-sized emulsion-based vehicle containing 13-cis-retinoic acid as a means of increasing its permeability and be a suitable topical therapy for acne. Various heterogeneous dispersions were formulated by spontaneous nano emulsification method using 9% w/w propylene glycol dicaprylate/dicaprate, 27% w/w caprylocaproyl macrogol glycerides, 9% w/w polyglyceryl–6–dioleate and 55% w/w distilled water as an external phase. All plain and 13- cis-retinoic acid loaded nanoemulsions were clear and showed suitable physicochemical parameters for desired topical delivery and stability. The permeation profiles of 13-cis-retinoic acid through rat skin from selected optimized nanoemulsion formulation followed zero order kinetics. The microscopic observations indicate that the optimized nanoemulsion has no significant effect on the microscopic structure of the skin and epithelial cells appeared mostly unchanged. The surface epithelium lining and the granular cellular structure of the skin were totally intact. Hence, developed nanoemulsion containing 13-cis-retinoic acid would be a potential drug delivery vehicle for effective management of acne.

Emulsions with alkyl polyglucosides as carriers for off-label topical spironolactone – safety and stability evaluation

Androgens play an important role in the pathogenesis of acne. Being an anti-androgen drug with many side effects, spironolactone has recently been used in dermatology as a topical therapy for acne. Off-label drug use in dermatology is common, although those drugs are basically available as compounded formulations; the choice of a proper vehicle is often neglected in that case. Alkyl polyglucosides (APGs) are a FDA certified class of polyethylene glycol (PEG)-free surfactants produced from the renewable resources. Following the preformulation tests, two different APG emulsifiers were used in this study to stabilize emulsions as carriers for topical spironolactone. Assessment of the physical stability of emulsions per se and after incorporation of 5% of spironolactone was performed using polarization microscopy, electrical conductivity and pH measurements. The skin irritation profile and moisturizing potential was assessed in vivo on human volunteers. APG-based emulsions per se and with 5% of spironolactone showed acceptable skin irritation profiles and significant potential for skin hydration, which is important in acne treatment. Good physical stability and satisfying preliminary safety profile of all investigated samples were also obtained showing that moisturizing APG-based emulsions could be promoted as vehicles for off-label topical spironolactone.

New technologies in topical acne therapy

The article is of an overview nature, it outlines the current understanding of the pathophysiology of acne, provides data on the role of retinoids in the treatment of dermatosis, discusses the advantages of combination therapy and new technologies in the treatment of acne.

Formulation development and evaluation of antiacne activity of ethosomal gel prepared using Plumbago zeylanica root extract

The objective of present research work is, to develop an ethosome, as a carrier system for Plumbago root extract, its incorporation into gel formulations and to characterize the developed gel formulations by estimation of plumbagin content and study of antiacne activity. Roots of Plumbago zeylanica L (Plumbaginaceae) contains Plumbagin and is used for skin infections and intestinal worms. Topical therapy for acne includes comedolytic agents, antibiotics and anti-inflammatory drugs. The excessive use of antibiotics has led to the increased resistance of acne-causing bacteria. In this research work, plumbago roots have been screened for their potential use for the treatment of acne and hydroalcoholic extract of the roots was found to be effective. Seven batches (EF1-EF7) of ethosomes were prepared using soya lecithin (1-3%) and ethanol (10-45%) and the hydroalcoholic extract. The range of entrapment efficiency varied from 17.12 to 80.82%. The ethosomes EF6 having highest entrapment efficiency was incorporated into gel formulation. Carbopol 934P (0.5 -2%) was used to prepare ethosomal gel and evaluated for physicochemical properties, drug content and diffusion characteristics. The pH of the gel was in the range of 6.87 to 7.03. Viscosity was between 5600 - 9800 centipoises. The % drug content was in the range of 95.91% to 100.7%. The ethosome, in their gel formulation, showed good physicochemical properties, drug content and diffusion pattern. The anti-acne activity of F3 showed good zones of inhibition comparable with standard Clindamycin. The present study suggested ethosomal gel as an efficient carrier for plumbago root extract for antiacne activity.

Ion Pair Strategy in Solid Lipid Nanoparticles: a Targeted Approach to Improve Epidermal Targeting with Controlled Adapalene Release, Resulting Reduced Skin Irritation.

Adapalene (AD) is one of the main retinoids used in the topical therapy of acne, an extremely common skin disease usually associated with psychological morbidity. However, like other retinoids, AD is frequently associated with skin irritation. To overcome the skin irritation, we proposed the encapsulation of AD in solid lipid nanoparticles (SLNs) using the ion pair strategy. The developed SLN-AD was characterized by high-performance liquid chromatography, differential scanning calorimetry, X-ray diffraction, synchrotron small-angle X-ray scattering, and transmission electron microscopy. In vitro permeation tests using porcine skin and in vivo mice skin irritation test were performed to evaluate, respectively, the drug's skin distribution and the skin irritation. The characterization studies were able to demonstrate that the proposed strategy effectively provided high AD encapsulation in SLNs and its incorporation into a hydrophilic gel. Sustained release, epidermal targeting, and less skin irritation were observed for SLN-AD gel in comparison to the marketed AD gel. The studies demonstrated that the encapsulation of AD in SLNs through the formation of an ion pair is a valuable alternative to diminish the adverse skin reactions caused by AD and can optimize patient adherence to treatment.

Formulation and Characterization of a 3D-Printed Cryptotanshinone-Loaded Niosomal Hydrogel for Topical Therapy of Acne.

Cryptotanshinone (CPT) is an efficacious acne treatment, while niosomal hydrogel is a known effective topical drug delivery system that produces a minimal amount of irritation. Three-dimensional (3D) printing technologies have the potential to improve the field of personalized acne treatment. Therefore, this study endeavored to develop a 3D-printed niosomal hydrogel (3DP-NH) containing CPT as a topical delivery system for acne therapy. Specifically, CPT-loaded niosomes were prepared using a reverse phase evaporation method, and the formulation was optimized using a response surface methodology. In vitro characterization showed that optimized CPT-loaded niosomes were below 150nm in size with an entrapment efficiency of between 67 and 71%. The CPT-loaded niosomes were added in a dropwise manner into the hydrogel to formulate CPT-loaded niosomal hydrogel (CPT-NH), which was then printed as 3DP-CPT-NH with specific drug dose, shape, and size using an extrusion-based 3D printer. The in vitro release behavior of 3DP-CPT-NH was found to follow the Korsmeyer-Peppas model. Permeation and deposition experiments showed significantly higher rates of transdermal flux, Q24, and CPT deposition (p < 0.05) compared with 3D-printed CPT-loaded conventional hydrogel (3DP-CPT-CH), which did not contain niosomes. In vivo anti-acne activity evaluated through an acne rat model revealed that 3DP-CPT-NH exhibited a greater anti-acne effect with no skin irritation. Enhanced skin hydration, wide inter-corneocyte gaps in the stratum corneum and a disturbed lipid arrangement may contribute towards the enhanced penetration properties of CPT. Collectively, this study demonstrated that 3DP-CPT-NH is a promising topical drug delivery system for personalized acne treatments.

An update on formulation strategies of benzoyl peroxide in efficient acne therapy with special focus on minimizing undesired effects.

Benzoyl peroxide (BPO) in the form of over the counter monotherapeutics or prescription-only combinations is a key component of topical acne therapy, but its unfavourable side effect profile reduces the therapeutic value of this compound. Various galenic approaches have been pursued to resolve this ambivalence, but only a few have managed to enter the market. This article aims to give a comprehensive overview of the published experimental vehicle systems and to identify the fundamental rationales. With regard to the formulation, an increase in the tolerability of BPO can essentially be achieved by combining BPO with re-fattening and moisturizing substances, by incorporating it and controlling its release, as well as by targeted deposition of the active ingredient at the site of action, i.e. drug targeting. Recently, novel particulate formulations have been proposed that combine several of these design principles and are expected to bring new developments in this dynamic field of research.

Bilosomes as a novel carrier for the cutaneous delivery for dapsone as a potential treatment of acne: preparation, characterization and in vivo skin deposition assay

In our study, the potential of bilosomes as novel vesicular carrier for the cutaneous delivery of the sulphone compound, Dapsone, for topical treatment of acne was investigated. The effect of different formulation variables (type and concentration of bile salt, and molar ratio of Span 60:cholesterol) on the properties of DPS-loaded bilosomes was investigated using a full factorial design. Design Expert software was used for data analysis and optimization of DPS-loaded bilosomes. The optimized bilosomes, chosen on the basis of their superior properties giving maximum entrapment, in vitro release after different time intervals and RE% with minimum vesicle size. Results showed that the bilosome system prepared using Span® 60: Cholesterol (5:1) and containing 0.25 M sodium deoxycholate as the bile salt was found to obey these criteria, with a desirability value of 0.637. Therefore, this system was chosen for further assessment for its morphological properties, zeta potential, thermal analysis using differential scanning calorimetry and X-ray diffractometry. Results revealed that the chosen bilosomes were spherical in shape with no aggregation, and contained DPS in a molecularly dispersed amorphous form. Finally, the capability of the optimized DPS-loaded bilosomes to deliver DPS through rat skin layers will be investigated and compared with that of DPS alcoholic solution. Results showed that the amounts of DPS retained in the skin treated with DPS-loaded bilosomes, and DPS alcoholic solution after 24 h were found to be 170.57 ± 55.12 and 120.24 ± 10.7 µg/mL, respectively, representing about 1.5-fold higher drug retained in the bilosomes-treated skin. Finally, the safety and the tolerability of the prepared bilosomes were assessed using histopathological examination, and revealed that the control untreated skin sections and skin sections treated with DPS-loaded bilosomes showed normal histological structures characterized by absence of defects or inflammation. Such results can be considered a good addition in the field of pharmaceutical drug delivery for effective topical therapy of acne.