FORMULATION AND IN VITRO SKIN PENETRATION OF A SOLID LIPID NANOPARTICLE GEL CONTAINING COFFEA ARABICA EXTRACT
Keywords:Coffea arabica, Microwave-assisted extraction, Solid lipid nanoparticle, Gel, Solid lipid nanoparticle gel, Physical stability
Objective: The extract of Coffea contains caffeine that could be used for its anticellulite activity. This study aimed to formulate a Coffea arabica
grounds residue extract into a solid lipid nanoparticles (SLNs) gel dosage form and examine the physical stability and in vitro skin penetration of the
Methods: Coffee grounds residue (CGR) extracts were made into three SLN formulations with different glycerin monostearate (GMS) concentrations
of 1%, 2%, and 3%. The SLN F2 formulation was a gel created by high-pressure homogenization (HPH). The in vitro penetration assessed using Franz
diffusion cells and the physical stability of the SLN extract gels was compared with those of the nonsense extract gel.
Results: Formulation F2 with 2% GMS had a mean particle size (PS) of 60.3 nm, a polydispersity index (PDI) of 0.278, and zeta potential of −32±1.40.
The PS for the SLN gel after HPH was 159 nm and the PDI was 0.211. Cycling and mechanical tests showed that the SLN gel was physically stable. The
cumulative amount of caffeine penetrated in vitro was 5.55±0.08 for the CGR-SLN gel and 4.18±0.08 for the CGR gel.
Conclusions: The amount of caffeine penetrated into rat skin was greater for the CGR-SLN gel than for the CGR gel.
Spent coffee grounds: A review on current research and future prospects.
Trends Food Sci Technol 2015;45:24-36.
2. Puglia C, Offerta A, Tirendi GG, Tarico MS, Curreri S, Bonina F, et al.
Design of solid lipid nanoparticles for caffeine topical administration.
Drug Deliv 2016;23:36-40.
3. Fadhila M, Mun’im A, Jufri M. A preparation, characterization, and
in vitro skin penetration of Morus alba root extract nanoemulsion.
Asian J Pharm Clin Res 2019;12:292-6.
4. Müller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN)
and nanostructured lipid carriers (NLC) in cosmetic and dermatological
preparations. Adv Drug Deliv Rev 2002;54:131-55.
5. Aland R, Ganesan M, Rajeswara RP. Development and optimization of
tazarotene loaded solid lipid nanoparticles for topical delivery. Asian J
Pharm Clin Res 2019;12:63-77.
6. Müller RH, Mäder K, Gohla S. Solid lipid nanoparticles (SLN) for
controlled drug delivery a review of the state of the art. Eur J Pharm
7. Sonawane R, Harde H, Katariya M, Agrawal S, Jain S. Solid lipid
Fig. 2: Cumulative penetration of caffeine from the coffee grounds
residue (CGR) gel and CGR-solid lipid nanoparticles gel through
rat skin nanoparticles-loaded topical gel containing combination drugs: An
approach to offset psoriasis. Expert Opin Drug Deliv 2014;11:1833-47.
8. Upadhyay R, Ramalakshmi K, Rao LJ. Microwave-assisted
extraction of chlorogenic acids from green coffee beans. Food Chem
9. Fajara BE, Susanti H. HPLC Determination of Caffeine in Coffee
Beverage. IOP Conference Series: Materials Science and Engineering;
10. Sangsen Y, Likhitwitayawuid K, Sritularak B, Wiwattanawongsa, K
Wiwattanapatapee R. Novel solid lipid nanoparticles for oral
delivery of oxyresveratrol effect of the formulation parameters on the
physicochemical properties and in vitro release. Int J Med Sci Eng
11. Khazaeli P, Pardakhty A, Shoorabi H. Caffeine-loaded niosomes:
Characterization and in vitro release studies. Drug Deliv 2007;14:447-52.
12. Ekambaram P, Abdul HS. Formulation and evaluation of solid lipid
nanoparticles of ramipril. J Young Pharm 2011;3:216-20.
13. Mappamasing F, Anwar E, Mun’im A. Formulasi, karakterisasi dan
uji penetrasi in vitro resveratrol solid lipid nanopartikel dalam krim
topikal (Formulation, characterization and in vitro penetration study
of resveratrol solid lipid nanoparticles in topical cream). J Ilmu
Kefarmasian Indones 2015;13:137-44.
14. Ramadon D, Wirarti GA, Anwar E. Novel transdermal ethosomal
gel containing green tea (Camellia sinensis L. Kuntze) leaves
extract: Formulation and in vitro penetration study. J Young Pharm
15. Avadi MR, Sadeghi AM, Mohammadpour N, Abedin S, Atyabi F,
Dinarvand R, et al. Preparation and characterization of insulin
nanoparticles using chitosan and Arabic gum with ionic gelation
method. Nanomedicine 2010;6:58-63.
16. Ghadiri M, Fatemi S, Vatanara A, Doroud D, Najafabadi AR, Darabi M,
et al. Loading hydrophilic drug in solid lipid media as nanoparticles:
Statistical modeling of entrapment efficiency and particle size. Int J
17. Sinko PJ. Physical chemical and biopharmaceutical principles in
the pharmaceutical sciences In: Martin’s Physical Pharmacy and
Pharmaceutical Sciences. Philadelphia, PA: Lippincott Williams and
Wilkins; 2011. p. 182-96.
18. Mazzafera P, Robinson SP. Characterization of polyphenol oxidase in
coffee. Phytochemistry 2000;55:285-96.
19. Bolzinger MA, Briançon S, Pelletier J, Fessi H, Chevalier Y.
Percutaneous release of caffeine from microemulsion, emulsion and gel
dosage forms. Eur J Pharm Biopharm 2008;68:446-51.
20. Notman R, Anwar J. Breaching the skin barrier--insights from molecular
simulation of model membranes. Adv Drug Deliv Rev 2013;65:237-50.