Title:Optimization and Transfollicular Delivery of Finasteride Loaded PLGA
Nanoparticles Laden Carbopol Gel for Treatment of Hair Growth
Stimulation
Volume: 20
Issue: 7
Author(s): Mounika Kuchukuntla*, Venkatesan Palanivel and Madhubabu Ananthula
Affiliation:
- Department of Pharmaceutical Science, Annamalai University, Annamalai Nagar, 608002, Tamil Nadu,
India
- Center for Nano medicine, Department of Pharmacy, Anurag University, Hyderabad, Telangana, 500088,
India
Keywords:
Finasteride, chemotherapy-induced alopecia, nano-precipitation method, box behnken design, JAK inhibitor, polymer matrix.
Abstract:
Background: One of the frequent side effects of cancer treatment is chemotherapyinduced
alopecia (CIA). The psychological discomfort of hair loss may cause patients to stop
receiving chemotherapy, lowering the therapy's effectiveness. Finasteride (FNS), a JAK inhibitor,
has shown tremendous promise in therapeutic uses for treating baldness. Still, systemic side
effects constrained its broad use in alopecia from oral treatment and a low absorption rate at
the target site-PLGA-loaded nanoparticles (NPs) for topical delivery of FNS-to overcome these
issues.
Methods: The nano-precipitation process was used to make FNS-NPs. The independent variables
(stabiliser and polymer) were PLGA (X1), P407 (X2), and sonication time (X3). Based on
the point prediction method obtainable by the Box Behnken design software, the best FNS-NPs
composition was selected. Entrapment efficiency, particle size, zeta potential, and polydispersity
index were used to characterize the nanoparticles. Using Carbopol as a polymer, the ideal
FNS-NPs composition was further transformed into a gel formulation. The prepared topical
gel formulation (FNS-NPs gel) included gel characterization, Dynamic Light Scattering
(DLS), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential
Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), in vitro and
in vivo studies.
Results: Optimized FNS-NPs (F13) had particle sizes of 175.26±3.85 nm, 0.241±0.11 PDI,
71.04±1.35 % EE, and -33.27±0.39 surface charges. There is no interaction between the drug and
the excipients, according to FTIR studies. The FNS were visible in the X-ray diffractogram enclosed
in a polymer matrix. The developed FNS-NPs gel formulation shows ideal drug content,
viscosity, pH, and spreadability. According to the release and permeation investigation findings,
FNS released slowly (68.73±0.94%) but significantly permeated the membrane more than before.
In a dose- and time-dependent manner, the produced nanoparticles considerably (p ≤0.05) increased
FNS delivery compared to the FNS solution. The FNS-NPs gel therapy significantly increases
the quantity and size of hair follicles dose-dependently. The effectiveness of the 1% FNSNPs
gel and the 2% minoxidil solution were comparable. After 72 hours, the FNS-NPs gel
showed no signs of skin irritation. The outcomes, therefore, showed that the trans follicular delivery
mechanism of the FNS-NPs gel might stimulate hair growth.
Conclusion: These findings imply that the innovative formulation that has been developed has several
beneficial properties that make it suitable for FNS dermal delivery in the treatment of alopecia areata.