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. 2023 Feb 6;9(2):135.
doi: 10.3390/gels9020135.

Development of Adapalene Loaded Liposome Based Gel for Acne

Asma Arooj  1 , Asim Ur Rehman  1 , Muhammad Iqbal  2 , Iffat Naz  3 , Aiyeshah Alhodaib  4 , Naveed Ahmed  1
Affiliations

Development of Adapalene Loaded Liposome Based Gel for Acne

Asma Arooj et al. Gels. .

Abstract

Retinoids are considered the mainstay treatment for moderate to severe acne. Adapalene, a third-generation retinoid, has physiochemical properties which hinder the effective delivery of the drug to the skin. Therefore, the current study aimed to develop and evaluate adapalene liposomal loaded gel (ADA-LP gel) for the effective management of acne to improve tolerability and delivery to targeted sites as compared to the conventional dosage form of the drug. A novel spontaneous phase transition method (SPT) was used to formulate liposomes. Liposomal formulation (ADA-LP) was prepared and optimized based on particle size, zeta potential, and PDI. Optimized formulation was further characterized by different techniques and loaded into Carbopol gel. In vitro drug release, ex vivo permeation, and in vivo studies were performed using the prepared adapalene-loaded liposomal-based gel. The in vivo study was done employing the testosterone-induced acne model in mice. The optimized formulation had a size of 181 nm, PDI 0.145, and a zeta potential of -35 mV, indicating that the formulation was stable. Encapsulation efficiency was 89.69 ± 0.5%. ADA-LPs were loaded into the gel. Prepared ADA-LP showed a 79 ± 0.02% release of drug in a sustained manner, within 24 h. The ex vivo permeability study showed a total of 43 ± 0.06 µg/cm2 of drug able to permeate through the skin within 24 h. Moreover, only 28.27 ± 0.04% was retained on the epidermis. The developed ADA-LP gel showed significant improvement in the acne lesions in mice with no visible scars and inflammation on the skin. Therefore, ADA-LP-based gel could be a promising carrier system for the safe and effective delivery of Adapalene.

Keywords: Carbopol; adapalene; animal model; liposomes; optimization; particle size.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
3D graphical representation of variables including PC, cholesterol, Tween 80 solution (%), and organic to aqueous ratio on responses particle size (a,b), zeta potential (c,d), and PDI (e,f).
Figure 2
Figure 2
(a) Particle size and PDI of LPs (b) Zeta potential of LPs. (c) Particle size and PDI of ADA-LP (d) Zeta potential of ADA-LPs.
Figure 3
Figure 3
(a) FTIR and (b) DSC of excipients, drug and prepared ADA-LP.
Figure 4
Figure 4
(a) 1% Carbopol blank gel. (b) Drug-loaded ADA-LP gel in 1% Carbopol.
Figure 5
Figure 5
Viscosity of ADA-LP gel measured at 25 °C.
Figure 6
Figure 6
In vitro release study at pH (a) 5.5, (b) 6.4, and (c) 7.4 where p = < 0.05.
Figure 7
Figure 7
(a) Ex vivo permeability of ADA-LP, ADA-LP gel, and marketed gel where p = <0.05 and (b) Drug deposition study in different skin layers.
Figure 8
Figure 8
Skin irritation study (a) positive control (b) negative control and (c) treatment with ADA-LP gel.
Figure 9
Figure 9
Testosterone-induced acne model in (a) normal group, (b) negative group, (c) positive group, and (d) treatment group after 3 weeks.
Figure 10
Figure 10
Testosterone-induced acne model in (a) normal groups, (b) negative group, (c) positive group, and (d) treatment group at the end of the study.
Figure 11
Figure 11
Histopathological analysis of (a) normal group, (b) negative group, (c) positive group, (d) treatment group.
See this image and copyright information in PMC

References

    1. Vos T., Flaxman A.D., Naghavi M., Lozano R., Michaud C., Ezzati M., Shibuya K., Salomon J.A., Abdalla S., Aboyans V. Years lived with disability (YLDs) for 1160 sequelae of 289 diseases and injuries 1990–2010: A systematic analysis for the Global Burden of Disease Study 2010. Lancet. 2012;380:2163–2196. doi: 10.1016/S0140-6736(12)61729-2. - DOI - PMC - PubMed
    1. Dreno B., Amici J.M., Demessant-Flavigny A.L., Wright C., Taieb C., Desai S.R., Alexis A. The impact of acne, atopic dermatitis, skin toxicities and scars on quality of life and the importance of a holistic treatment approach. Clin. Cosmet. Investig. Dermatol. 2021;14:623. doi: 10.2147/CCID.S315846. - DOI - PMC - PubMed
    1. Akel H., Ismail R., Katona G., Sabir F., Ambrus R., Csóka I. A comparison study of lipid and polymeric nanoparticles in the nasal delivery of meloxicam: Formulation, characterization, and in vitro evaluation. Int. J. Pharm. 2021;604:120724. doi: 10.1016/j.ijpharm.2021.120724. - DOI - PubMed
    1. Afzal M., Alharbi K.S., Alruwaili N.K., Al-Abassi F.A., Al-Malki A.A.L., Kazmi I., Kumar V., Kamal M.A., Nadeem M.S., Aslam M. Seminars in Cancer Biology. Academic Press; Cambridge, MA, USA: 2021. Nanomedicine in treatment of breast cancer—A challenge to conventional therapy; pp. 279–292. - PubMed
    1. Khattak M.I.K., Ahmed N., Umer M.F., Riaz A., Ahmad N.M., Khan G.M. Chloroform-Injection (CI) and Spontaneous-Phase-Transition (SPT) Are Novel Methods, Simplifying the Fabrication of Liposomes with Versatile Solution to Cholesterol Content and Size Distribution. Pharmaceutics. 2020;12:1065. doi: 10.3390/pharmaceutics12111065. - DOI - PMC - PubMed