Tretinoin-loaded liposomal formulations: from lab to comparative clinical study in acne patients

Rahman, Salwa Abdel; Abdelmalak, Nevine Shawky; Badawi, Alia; Elbayoumy, Tahany; Sabry, Nirmeen A.; Ramly, Amany El

doi:10.3109/10717544.2015.1041578

Cited by 43 publications

(27 citation statements)

References 42 publications

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“…Little changes in the skin structure were observed in the Prilox-treated skin as can be seen from the photograph. The skin histopathology examination indicated the biocompatible nature of the optimized MMNG formulations, and hence, the formulations indicated to be well tolerated by skin (34,49,50).…”

Section: Skin Compliance Studiesmentioning

confidence: 97%

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

et al. 2016

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The topical delivery of local anaesthetics has always been a difficult task due to the limited percutaneous absorption of local anaesthetic drugs across the various barriers of the skin. In this pursuit, a thermoresponsive mixed micellar nanogel (MMNG) system of lidocaine and prilocaine has been attempted in the current piece of work. The system relies on the ability to alter its phase state (sol-to-gel) for feasibility of the topical application in response to change in temperature. The composition of MMNG entails majorly of Pluronic® F127 and Tween 80 in a fixed combination so as to provide the desired thermoreversibility for the skin application. The gels were optimized with respect to phase transition temperature (T ), turbidity and viscosity. The optimized systems were then characterized for particle size, spreadability, syringeability, bioadhesive strength, ex vivo skin permeation, retention and dermatokinetic studies. The skin compatibility revealed that no histological changes were observed for optimized formulation, while the conventional system showed changes in the skin-tissues. Further, the enhanced intensity of anaesthetic effect was noted in an in vivo rabbit model and tail flick model in mice. The overall results suggest that the prepared MMNG system possesses the potential in providing an efficacious, safe and acceptable alternative therapeutic system for topical anaesthesia.

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Section: Skin Compliance Studiesmentioning

confidence: 97%

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

et al. 2016

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“…These are related to: (1) increased bioavailability; (2) decreased toxicity and skin irritation; (3) increased in vivo half-life; (4) increased RA photostability; (5) increased cell targeting and capacity to cross biological barriers. The advantages of RA formulations have been demonstrated in preclinical (in all applications described in this review) and clinical trials (cancer and skin applications) 71,129 . In the case of cancer, recent studies indicate that the antitumoral activity of RA might be greatly enhanced with formulations that extend the in vivo half-life of RA 12 .…”

Section: Future Outlookmentioning

confidence: 99%

“…Others were tested in clinical trials but did not reach the market. For example, a liposomal-based formulation of RA (monotherapy) was successfully tested in patients with facial acne 71 and refractory hematological malignancies in a phase II clinical trial 70 . In the last application, the remission rate (67% clinical remission) was lower than that obtained using a combinatorial therapy (77% clinical remission), which included oral administration of ATRA plus idarubicin and thus the liposomal formulation was not further evaluated.…”

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confidence: 99%

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Advances and challenges in retinoid delivery systems in regenerative and therapeutic medicine

et al. 2020

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Retinoids regulate a wide spectrum of cellular functions from the embryo throughout adulthood, including cell differentiation, metabolic regulation, and inflammation. These traits make retinoids very attractive molecules for medical purposes. In light of some of the physicochemical limitations of retinoids, the development of drug delivery systems offers several advantages for clinical translation of retinoid-based therapies, including improved solubilization, prolonged circulation, reduced toxicity, sustained release, and improved efficacy. In this Review, we discuss advances in preclinical and clinical tests regarding retinoid formulations, specifically the ones based in natural retinoids, evaluated in the context of regenerative medicine, brain, cancer, skin, and immune diseases. Advantages and limitations of retinoid formulations, as well as prospects to push the field forward, will be presented. R etinoic acid (RA) signaling is one of the most important biological pathways in nature, triggered by RA interaction with nuclear receptors that control gene expression. The chemical structure of retinol (vitamin A, a RA precursor) was first described by Paul Karrer in 1931 1 , who was awarded a Nobel Prize in 1937 for the discovery. The use of RA for skin disorders 2 and cancer treatment (acute myeloid leukemia (AML) 3 and cervical neoplasia 4,5) started in the 1960s and 1980s (Fig. 1). By the 2000s, RA had been incorporated in many tissue engineering scaffolds as a stem cell differentiation agent 6,7. Over the last 10 years, many discoveries related to the biological role of RA in controlling the biology of hematopoietic stem cells 8,9 , tumor-initiating cells 10-12 , immune cells 13 , intestinal mucosa wound repair 14 , cancer resistance 15 , and cell reprogramming and differentiation 16,17 , have further stimulated the interest in this drug for many other biomedical applications. This interest is confirmed by more than 50 active clinical trials (according to ClinicalTrials.gov) evaluating the effect of RA in cancer (28 trials), mostly in hematological (16 trials) and brain tumors (8 trials), skin pathologies (e.g., acne, photoaging, eczema) (5 trials), and in other conditions such as inflammation, olfactory loss, and neuropsychiatric diseases (Table 1). Clinical applications of RA have highlighted three main limitations of its pharmacological use. First, RA is poorly soluble in aqueous solutions 18 and photosensitive 19 , which makes its administration challenging. Secondly, RA induces irritation when applied onto the skin and increases its catabolism, when it is administered intravenously, reducing its therapeutic efficacy 20. Lastly, RA is involved in many biological processes and thus the systemic delivery of RA causes side effects. All these limitations motivated researchers to synthesize novel and

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“…Photosensitive nanoformulations are also applied in acne treatment, a common inflammatory skin condition that can cause discomfort and visible, long-lasting scarring [127]. Examples of treatment agents for acne lesions are retinoids, such as tretinoin, efficiently encapsulated in liposomes [102] and nanoemulsions [110]. In clinical studies, the formulations result in a reduced number of acne lesions and improved skin condition with high efficacy.…”

Section: Advances In Skin Formulationsmentioning

confidence: 99%

Recent Advances in the Structural Design of Photosensitive Agent Formulations Using “Soft” Colloidal Nanocarriers

et al. 2020

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The growing demand for effective delivery of photosensitive active compounds has resulted in the development of colloid chemistry and nanotechnology. Recently, many kinds of novel formulations with outstanding pharmaceutical potential have been investigated with an expansion in the design of a wide variety of “soft” nanostructures such as simple or multiple (double) nanoemulsions and lipid formulations. The latter can then be distinguished into vesicular, including liposomes and “smart” vesicles such as transferosomes, niosomes and ethosomes, and non-vesicular nanosystems with solid lipid nanoparticles and nanostructured lipid carriers. Encapsulation of photosensitive agents such as drugs, dyes, photosensitizers or antioxidants can be specifically formulated by the self-assembly of phospholipids or other amphiphilic compounds. They are intended to match unique pharmaceutic and cosmetic requirements and to improve their delivery to the target site via the most common, i.e., transdermal, intravenous or oral administration routes. Numerous surface modifications and functionalization of the nanostructures allow increasing their effectiveness and, consequently, may contribute to the treatment of many diseases, primarily cancer. An increasing article number is evidencing significant advances in applications of the different classes of the photosensitive agents incorporated in the ”soft” colloidal nanocarriers that deserved to be highlighted in the present review.

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Tretinoin-loaded liposomal formulations: from lab to comparative clinical study in acne patients

Cited by 43 publications

References 42 publications

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

Advances and challenges in retinoid delivery systems in regenerative and therapeutic medicine

Recent Advances in the Structural Design of Photosensitive Agent Formulations Using “Soft” Colloidal Nanocarriers

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