Development and optimization of a tamsulosin nanostructured lipid carrier loaded with saw palmetto oil and pumpkin seed oil for treatment of benign prostatic hyperplasia.

Benign prostatic hyperplasia (BPH) is a nonmalignant growth of the prostate tissue and causes urinary tract symptoms. To provide effective treatment, tamsulosin (TM), saw palmetto oil (SP), and pumpkin seed oil (PSO) were combined and fabricated a nanostructured lipid carrier (NLC) as TM-S/P-NLC using experimental design. The purpose was to enhance the permeation and therapeutic activity of TM; combining TM with SP and PSO in an NLC generates a synergistic activity. An optimized TM-S/P-NLC was obtained after statistical analysis, and it had a particle size, percentage of entrapment efficiency, and steady-state flux of 102 nm, 65%, and 4.5 µg/cm2.min, respectively. Additionally, the optimized TM-S/P-NLC had spherical particles with a more or less uniform size and a stability score of 95%, indicating a high level of stability. The in vitro release studies exhibited the optimized TM-S/P-NLC had the maximum release profile for TM (81 ± 4%) as compared to the TM-NLCs prepared without the addition of S/P oil (59 ± 3%) or the TM aqueous suspension (30 ± 5%). The plasma TM concentration-time profile for the TM-S/P-NLC and the marketed TM tablets indicated that when TM was supplied in a TM-S/P-NLC, the pharmacokinetic profile of the drug was improved. Simultaneously, in vivo therapeutic efficacy studies also showed favorable results for the TM-S/P-NLC in terms of the prostate weight and prostate index following treatment of BPH. Based on the findings of present study, we suggest that in the future, the TM-S/P-NLC could be a novel drug delivery system for treating BPH.

Finasteride nano-transferosomal gel formula for management of androgenetic alopecia: ex vivo investigational approach.

INTRODUCTION: Finasteride (FIN) is known as type II 5α-reductase inhibitor, which has been approved for the treatment and prevention of androgenetic alopecia. Administration of FIN by oral route has led to undesirable systemic side effects that include mood disturbance, gynecomastia, decreased libido, erectile dysfunction, and ejaculation disorder. The aim was to improve FIN delivery through skin layers and hair follicles that could possibly reduce its major side effects resulting from long-term oral administration for the treatment and prevention of male pattern baldness. MATERIALS AND METHODS: FIN was formulated as nano-transferosomal (NTF) gel formulations (F1-3). The prepared formulations were characterized for encapsulation efficiency, particle size, ex vivo skin permeation, and kinetic modeling. In addition, visualization of NTF skin penetration using a fluorescence laser microscope was carried out for the selected formula (F2). RESULTS AND DISCUSSION: The results showed that FIN encapsulation efficiency percentage was 69.72 ± 8.36, 89.43 ± 6.82, and 93.1 ± 1.93 for F1, F2, and F3, respectively. FIN-NTF average vesicle sizes were 299.6 ± 45.6, 171 ± 25.6, and 197.4 ± 29.1 nm for F1, F2, and F3, respectively. FIN-NTF formulations (F1-3) showed enhancement and improvement in the amount of FIN permeated compared with raw FIN gel formula. The NTF formula revealed uniform fluorescence (rhodamine) intensity across rat skin, which indicated improved delivery through skin layers compared with control gel formula. CONCLUSION: These results indicated that NTF gel formula showed the ability to boost FIN delivery across skin layers and could be applied as an alternative for oral therapy.