Thin Film Hydration Method Research Articles

Design optimization of Fucoidan-coating Cationic Liposomes for enhance Gemcitabine delivery.

Obstacles facing chemotherapeutic drugs for cancers led scientists to load Gemcitabine (GEM) into nanocarriers like liposomes, known for their nontoxicity profile and targeting capacity. The liposomal nanostructures containing GEM were coated with Fucoidan (FU) due to its anti-tumor properties by targeting cancer cells. Thus four different cationic liposomes formulations were prepared by thin-film hydration method in optimal conditions: DOTAP (formulation A); DPPC/DOTAP (4:1 molar ratio, formulation B), DPPC/DMPC/DOTAP (4:1:1 molar ratio, formulation C) and DPPC/DMPC/DOTAP/DSPE-mPEG2000 (4:1:1:0.1 molar ratio, formulation D). They were studied to identify lipid-compositions offering effective GEM-entrapment and successful coating of FU on the liposome surface. Additional qualitative characteristics, such as particle size, polydispersity index, zeta potential, stability and in vitro drug release were then evaluated. Formulation C gave the best GEM-entrapment efficiency (EE) but formed aggregates when coated with FU, giving non-homogenous large size particles then not suitable for effective delivery. It was the same situation with formulation A and B. Only the formulation D showed a good GEM-EE (> 80%) and affinity by successful coating FU from three different algae species. The PEGylated formulation D coated of FU, with regard to storage stability and drug release studies, revealed to be a promising approach on design of optimal drug delivery system.

Effect of size and pH-sensitivity of liposomes on cellular uptake pathways and pharmacokinetics of encapsulated gemcitabine

To enhance cytoplasmic delivery efficiency, pH-sensitive liposomes (PSL) have been proposed as a novel strategy. To facilitate clinical translation, this study aims to understand the impact of both size and pH-sensitivity on cellular uptake pathways, intracellular trafficking and pharmacokinetics of liposomes. The large liposomes (130-160 nm) were prepared using thin-film hydration method, while small liposomes (∼60 nm) were fabricated using microfluidics, for both PSL and non-pH-sensitive liposomes (NPSL). Cellular uptake pathways and intracellular trafficking was investigated through confocal imaging with aid of various endocytosis inhibitors. Intracellular gemcitabine delivery by various liposomal formulations was quantified using HPLC, and the cytotoxicity was assessed via cell viability assays. Pharmacokinetics of gemcitabine loaded in various liposomes was evaluated in rats following intravenous administration. Larger liposomes had a higher loading capacity for hydrophilic gemcitabine (7% vs 4%). Small PSL exhibited superior cellular uptake compared to large PSL or NPSLs. Moreover, the alkalization of endosomes significantly attenuated the cellular uptake of PSL. Large liposomes (PSL and NPSL) predominantly entered cells via clathrin-dependent pathway, whereas small liposomes partially utilized caveolae-dependent pathway. However, the long circulation of the liposomes, as measured by the encapsulated gemcitabine, was compromised by both pH-sensitivity and size reduction (9.5 h vs 5.3 h). Despite this drawback, our results indicate that small PSL holds promise as vectors for the next generation of liposomal nanomedicine, owing to their superior cytoplasmic delivery efficiency.

Development and characterization of Decitabine Niosomes

The present study was focused on formulating and evaluating Decitabine containing niosomes formulation for In Vitro studies. Niosomal formulations were prepared by using different ratio of surfactant (Tween 80 and Tween 20) and cholesterol by thin film hydration method and were evaluated for In Vitro characteristics, stability studies. Span 20 containing niosomal formulation displayed highest entrapment efficiency with desired particle size. SEM analyses showed that niosomal formulation was spherical in shape. Niosomes containing Tween 20 displayed higher percentage of drug release after 8 h as compared to other formulations. F-7 formulation was found to be stable at the end of the study on storage condition. The present study suggested that niosomal formulations provide sustained and prolonged delivery of drug with enhance bioavailability.

Curcumin and Baicalin Co-Loaded Nanoliposomes for Synergistic Treatment of Non-Small Cell Lung Cancer.

Currently, the treatment of patients with advanced non-small cell lung cancer (NSCLC) mainly relies on traditional chemotherapeutic drugs; however, most of them have limited therapeutic effects and high toxicity. Some natural products with good therapeutic efficacy and low toxicity and side effects are limited in clinical application due to their low solubility and bioavailability. In this study, a nanoliposome drug-carrying system (Lip-Cur/Ba) was developed for the co-delivery of curcumin (Cur) and baicalin (Ba) using the thin-film hydration method. In vitro experiments demonstrated that Lip-Cur/Ba had a strong killing effect on A549 cells, and the inhibitory effect of Lip-Cur/Ba on A549 cells was enhanced by 67.8% and 51.9% relative to that of the single-carrier system, which could reduce the use of a single-drug dose (Lip-Cur and Lip-Ba), delay the release rate of the drug and improve the bioavailability. In vivo experiments demonstrated the antitumor activity of Lip-Cur/Ba by intravitreal injection in BALB/c mice, and there were no obvious toxic side effects. This study provides a new idea for curcumin and baicalin to be used in the co-treatment of NSCLC by constructing a new vector.

Fluconazole-Niosome-Laden Contact Lens: A Promising Therapeutic Approach for Prolonged Ocular Delivery and Enhanced Antifungal Activity

BackgroundTraditional routes of administration of fluconazole such as eye drops have a low therapeutic efficacy due to insufficient bioavailability.PurposeHerein, a fluconazole noisome-laden contact lens was prepared to control and prolong the drug release and improve its bioavailability.MethodsTwo methods have been used to prepare fluconazole niosomes: solvent injection method and thin film hydration method utilizing span 60 and cholesterol mixture. Subsequently, formulations were optimized using three factors and a two-level factorial design and were subjected to in-vitro characterization for the size of niosomes, zeta potential, entrapment efficiency percent, and cytotoxicity study. The optimized fluconazole niosomes were further entrapped in contact lenses by the soaking method and were evaluated according to in-vitro release profile, and antimicrobial activity.ResultsThe results revealed that the investigated fluconazole niosomes are of nano-size ranging from 228.2 to 769.2 nm with zeta-potential values between − 18.1 and − 60.2 mV. The entrapment efficiency percentage ranged from 51.3 to 75%. Fluconazole was released from fluconazole noisome-laden contact lens and showed a prolonged release up to 48–72 h with a cumulative release of 79.62%. Statistical analysis showed that fluconazole-noisome-laden contact lenses have a significant impressive fungal adhesion reduction as compared to fluconazole-laden contact lenses.ConclusionFluconazole noisome-laden contact lenses are a promising therapeutic way for effective and prolonged treatment of ocular fungal infection.

Development and evaluation of curcumin-loaded vesicular carriers: impact of formulation variables

Vesicular carriers are a well-established approach to improving the technological and biopharmaceutical characteristics of the loaded cargo. The current manuscript is focused on the development and evaluation in a comparative aspect of two types of vesicles—ethosomes and transfersomes loaded with the phytoconstituent curcumin. The formulation variables affecting their physiochemical and cytotoxic properties are outlined as well. A series of ethosomes and transfersomes based on Lipoid S75 and ethanol, or edge activator, were prepared using the thin film hydration method and subjected to comprehensive evaluation by dynamic light scattering (DLS) analysis, transmission electron microscopy (TEM), entrapment efficiency evaluation, in vitro release, and cytotoxicity studies. Ethosomes based on Lipoid S75 (4% w/w) and ethanol (30% v/v) showed suitable physicochemical characteristics (hydrodynamic diameter of 578.6 nm, monomodal size distribution, high curcumin entrapment efficiency (78.2%)), and superior antiproliferative activity compared to free drug and transfersomal nanocarriers.

Intranasal bilosomes in thermosensitive hydrogel: advancing desvenlafaxine succinate delivery for depression management

Depression, the second biggest cause of disability worldwide, is widespread. Many antidepressant medications, including Desvenlafaxine Succinate (D.V.S.), function by elevating neurotransmitter levels at the synapse through the inhibition of reabsorption by neurons. However, the effectiveness of these treatments is often limited by their inability to reach the brain using conventional administration methods. Bilosome-stabilized nanovesicles containing bile salts have drawn much interest because of their adaptability and versatility in various applications. This study aimed to address this issue by formulating intranasal bilosomes incorporated into a mucoadhesive in situ gel to deliver D.V.S. directly to the brain for depression treatment. The desvenlafaxine-loaded bilosomes were developed using a thin film hydration method based on the l-optimal design. They were intended to provide a more convenient route of administration for antidepressants, enhancing bioavailability and brain targeting through intranasal delivery. The study assessed the optimized bilosomes for particle size (311.21 ± 0.42 nm), Zeta potential (–37.35 ± 0.43)and encapsulation efficiency (99.53 ± 0.41%) and further evaluated them in ex vivo and in vivo pharmacokinetics studies. Pharmacokinetic data reveal enhanced brain uptake compared to a free drug. A statistically optimized bilosome formulation was determined. The intranasal administration of mucoadhesive in situ gel containing desvenlafaxine succinate-loaded bilosomes facilitated direct nose-to-brain drug delivery, improving brain bioavailability.

Codelivery of methotrexate and silibinin by niosome nanoparticles for enhanced chemotherapy of CT26 colon cancer cells

Colon cancer (CC) is one of the most prevalent cancers in the world, and chemotherapy is widely applied to combat it. However, chemotherapy drugs have severe side effects and emergence of multi drug resistance (MDR) is common. This bottleneck can be overcome by niosome nanocarriers that minimize drug dose/toxicity meanwhile allow co-loading of incompatible drugs for combination therapy. In this research, silibinin (Sil) as a hydrophobic drug was loaded into the lipophilic part, and methotrexate (MTX) into the hydrophilic part of niosome by the thin film hydration (TFH) method to form Nio@MS NPs for CT26 colon cancer therapy in vitro. Our results indicated synthesis of ideal niosome nanoparticles (NPs) with spherical morphology, size of ∼100 nm, and a zeta potential of −10 mV. The IC50 value for Nio@MS was determined ∼2.6 µg ml−1, which was significantly lower than MTX-Sil (∼6.86 µg ml−1), Sil (18.46 µg ml−1 ), and MTX (9.8 µg ml−1 ). Further, Nio@MS significantly reduced cell adhesion density, promoted apoptosis and increased gene expression level of caspase 3 and BAX while promoted significant downregulation of BCL2. In conclusion, the design and application of niosome to co-administer Sil and MTX can increase the drugs cytotoxicity, reduce their dose and improve anti-cancer potential by combating MDR.

Dual-targeting liposomes modified with BTP-7 and pHA for combined delivery of TCPP and TMZ to enhance the anti-tumour effect in glioblastoma cells

Aim To construct a novel nano-carrier with dual ligands to achieve superior anti-tumour efficacy and lower toxic side effects. Methods Liposomes were prepared by thin film hydration method. Ultraviolet, high performance liquid chromatography, nano-size analyser, ultrafiltration centrifugation, dialysis, transmission electron microscope, flow cytometry, Cell Counting Kit-8, confocal laser scanning microscopy, transwell, and tumorsphere assay were used to study the characterisations, cytotoxicity, and in vitro targeting of dg-Bcan targeting peptide (BTP-7)/pHA-temozolomide (TMZ)/tetra(4-carboxyphenyl)porphyrin (TCPP)-Lip. Results BTP-7/pHA-TMZ/TCPP-Lip was a spheroid with a mean diameters of 143 ± 3.214 nm, a polydispersity index of 0.203 ± 0.025 and a surface charge of −22.8 ± 0.425 mV. The drug loadings (TMZ and TCPP) are 7.40 ± 0.23% and 2.05 ± 0.03% (mg/mg); and the encapsulation efficiencies are 81.43 ± 0.51% and 84.28 ± 1.64% (mg/mg). The results showed that BTP-7/pHA-TMZ/TCPP-Lip presented enhanced targeting and cytotoxicity. Conclusion BTP-7/pHA-TMZ/TCPP-Lip can specifically target the tumour cells to achieve efficient drug delivery, and improve the anti-tumour efficacy and reduces the systemic toxicity.

Quality by Design-Steered Development of Stealth Liposomal Formulation of Everolimus: A Systematic Optimization and Evaluation.

Everolimus is a drug approved for the treatment of breast cancer with HR+ and advanced breast cancer reoccurring in postmenopausal women. The oral administration of EVE has been observed to have low oral bioavailability and severe epithelial cutaneous events that include rashes and lip ulceration followed by mouth ulceration after oral administration. The present research aimed to enhance the bioavailability by loading the EVE into a stealth liposomal formulation (S-EVE-LIPO) intended for intravenous administration. The surface of the liposomes was modified with vitamin E TPGS, which prolongs the systemic circulation of the drug and provides additional benefits like inhibition of the P-gp efflux pump and acting synergistically with EVE. The formulation was prepared using the thin film hydration method and optimized using a D-optimal mixture design. ANOVA suggested the significance of the proposed mathematic model, and the optimized formulation was generated by design expert software. The optimized formulation (S-EVE-LIPO) was observed with nanometric size (99.5 ± 3.70 nm) with higher encapsulation efficacy (81.5 ± 2.86 %). The S-EVELIPO formulation indicated a sustained release profile as 90.22% drug release was observed in 48 h, whereas the formulation without vitamin E TPGS (EVE-LIPO) released only 74.15 drugs in 24 hours. In vitro cytotoxicity study suggested that the presence of vitamin E TPGS lowers the IC50 value (54.2 ± 1.69), increases the cellular uptake of the formulation, also increases the generation of ROS, and shows better hemocompatibility. Vitamin E TPGS could be set as a vital additive to improve therapeutic efficacy and reduce offsite toxicity and dosing frequency.

Synthesis, Characterization, and In-Vitro Evaluation of Silibinin-loaded PEGylated Niosomal Nanoparticles: Potential Anti-Cancer Effects on SW480 Colon Cancer Cells.

Colorectal cancer is a significant global health concern with high mortality rates. Silibinin is a compound derived from milk thistle with anticancer properties and may be a potential treatment option for colorectal cancer. Its poor solubility limits its clinical application, but various strategies, such as nanoparticle encapsulation, have shown promise. In this study, a PEGylated niosomal drug delivery system was used to enhance the solubility of silibinin, and its anti-proliferative effects were evaluated against human colorectal cancer cell lines. The silibinin-loaded PEGylated niosomal nanoparticles (NIO-SIL) were fabricated using the thin-film hydration method and characterized with dialysis bag, AFM, SEM, DLS, and FTIR systems. Finally, the cancerous cells and human normal cells were treated with NIO-SIL and pure silibinin. The proliferation, apoptosis, and cell cycle of these cells were evaluated. Subsequently, the expression of Bax, Bcl-2, p53, and cyclin D1 genes was measured using real-time PCR. The drug release profile, size, morphology, and chemical interactions of the synthesized PEGylated niosomal nanoparticles were suitable for use as a drug delivery system. Both pure silibinin and NIO-SIL could reduce the proliferation of cancerous cells, induce apoptosis, and cause cell cycle arrest, with no significant negative effects reported on human normal cells. Both pure silibinin and NIO-SIL reduced the expression of the Bcl-2 and cyclin D1 genes while increasing the expression of Bax and p53. (p-value < 0.05 *). The outcomes of this study indicate the high potential of PEGylated niosomal nanoparticles for encapsulation and delivery of silibinin to cancer cells, with no negative effects on normal cells.

Production of Targeted Estrone Liposomes Using a Herringbone Micromixer.

Liposomes are spherical vesicles formed from bilayer lipid membranes that are extensively used in targeted drug delivery as nanocarriers to deliver therapeutic reagents to specific tissues and organs in the body. Recently, we have reported using estrone as an endogenous ligand on doxorubicin-encapsulating liposomes to target estrogen receptor (ER)-positive breast cancer cells. Estrone liposomes were synthesized using the thin-film hydration method, which is a long, arduous, and multistep process. Here, we report using a herringbone micromixer to synthesize estrone liposomes in a simple and rapid manner. A solvent stream containing the lipids was mixed with a stream of phosphate buffer saline (PBS) inside a microchannel integrated with herringbone-shaped ridges that enhanced the mixing of the two streams. The small scale involved enabled rapid solvent exchange and initiated the self-assembly of the lipids to form the required liposomes. The effect of different parameters on liposome size, such as the ratio between the flow rate of the solvent and the buffer solutions (FRR), total flow rate, lipid concentrations, and solvent type, were investigated. Using this commercially available chip, we obtained liposomes with a radius of 66.1 ± 11.2 nm (mean ± standard deviation) and a polydispersity of 22% in less than 15 minutes compared to a total of ∼ 11 hours using conventional techniques. Calcein was encapsulated inside the prepared liposomes as a model drug and was released by applying ultrasound at different powers. The size of the prepared liposomes was stable over a period of one month. Overall, using microfluidics to synthesize estrone liposomes simplified the procedure considerably and improved the reproducibility of the resulting liposomes.

Novel Proniosomes of Manidipine: Optimization and In-vivo Evaluation

The objective of the current study is to produce proniosomes of manidipine using the thin film hydration method for the management of hypertension. Statistical optimization was performed using the Box-Behnken design. The generated formulations were tested for particle size, entrapment effectiveness, and drug release at 12 hours. The improved proniosomes were further assessed for surface morphology, ATR, and differential scanning calorimetry (DSC). The improved proniosomes were also assessed for an in-vitro and in-vivo investigation on dexamethasone-induced hypertension. It was noted that there was no significant interaction with excipients. DSC indicated a considerable shift in the endothermal peak and showed interaction with the study’s excipients. Niosomes and drug crystals were seen to be dispersed in small areas during the scanning electron microscope (SEM) analysis. The study also showed that the optimized proniosomes have asymmetrical surfaces and appearances. The zeta value in the research was -6.7 mV, indicating stability. According to the optimized proniosomes formulation, F14 released 99.97% of the drug at its highest concentration in 12 hours. ANOVA results from an in-vivo investigation confirmed a satisfactory outcome in decreasing raised blood pressure, as shown by the F and p-values.

Green synthesis and characterization of AgNPs, liposomal loaded AgNPs and ZnPcS4 photosensitizer for enhanced photodynamic therapy effects in MCF-7 breast cancer cells

Breast cancer remains a formidable challenge in oncology despite significant advancements in treatment modalities. Conventional therapies such as surgery, chemotherapy, radiation therapy, and hormonal therapy have been the mainstay in managing breast cancer for decades. However, a subset of patient's experiences treatment failure, leading to disease recurrence and progression. Therefore, this study investigates the therapeutic potential of green-synthesized silver nanoparticles (AgNPs) using an African medicinal plant (Dicoma anomala methanol root extract) as a reducing agent for combating breast cancer. AgNPs were synthesized using the bottom-up approach and later modified with liposomes (Lip) loaded with photosensitizer (PS) zinc phthalocyanine tetrasulfonate (Lip@ZnPcS4) using thin film hydration method. The successful formation and Lip modification of AgNPs, alongside ZnPcS4, were confirmed through various analytical techniques including UV–Vis spectroscopy, Fourier-transform infrared spectroscopy (FT-IR), high-resolution transmission electron microscopy (HR-TEM), scanning electron microscopy (SEM) and energy dispersive X-ray spectroscopy (EDS). Following a 24 h treatment period, MCF-7 cells were assessed for viability using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT viability assay), cell death analysis using mitochondrial membrane potential (MMP) (ΔΨm), Annexin V-fluorescein isothiocyanate (FITC)-propidium iodide (PI) kit, and caspase- 3, 8 and 9 activities. The experiments were repeated four times (n = 4), and the results were analyzed using SPSS statistical software version 27, with a confidence interval set at 0.95. The synthesized nanoparticles and nanocomplex, including AgNPs, AgNPs-Lip, Lip@ZnPcS4, and AgNPs-Lip@ZnPcS4, exhibited notable cytotoxicity and therapeutic efficacy against MCF-7 breast cancer cells. Notably, the induction of apoptosis, governed by the upregulation of apoptotic proteins i.e., caspase 8 and 9 activities. In addition, caspase 3 was not expressed by MCF-7 cells in both control and experimental groups. Given the challenging prognosis associated with breast cancer, the findings underscore the promise of liposomal nanoformulations in cancer photodynamic therapy (PDT), thus warranting further exploration in clinical settings.

Development of thermosensitive liposome-containing in-situ gel systems for intranasal administration of thiocolchicoside and in vivo evaluation in a rabbit model

Aim Thiocolchicoside (THC) is a drug under the category of BCS III. Due to its high molecular weight, it has poor oral bioavailability and low skin permeability. This study aims to find an alternative delivery method for THC that enhances its bioavailability through nasal application approach. In situ gels containing plain or liposomal THC with different combinations of Pluronic® F127 and PEG 400 were prepared. Method Liposome formulations were prepared using the thin film hydration method and tested for their characterization such as for drug content, particle size, and zeta potential. In vivo pharmacokinetic parameters of formulations such as Cmax, Tmax, and AUC were tested on the rabbit model. The formulations were also scrutinized for their cell viability properties. Result Formulation composition with 2% soybean phosphatidylcholine and 10 mg THC exhibited ∼94% entrapment efficiency, minimum particle size 101.32 nm, low polydispersity index 0.225 and +0.355 zeta potential. In situ liposomal dispersion containing 15% Pluronic® F127 turned into gel at nasal temperature. Cell lines were unharmed for 48 h. İn situ liposomal gels showed 1.5x higher blood concentration than the control formula. Conclusion In situ gels of liposomal THC formulations offer advantages over traditional nasal solutions, demonstrating comparable bioavailability to parenteral medication while also preserving the health of nasal mucosa cells.

Improved Topical Antifungal Medication using Sertaconazole Bilosomes: In vitro Permeability, Cytotoxicity, and Clinical Assessment

Objective: The purpose of the current study was to develop Sertaconazole bilosomes (SBs) with enhanced permeability, skin deposition, anti-fungal properties, and clinical efficacy. Methods: By changing span 60 to cholesterol molar ratio, bile salt type, and concentration, 12 formulations of SBs were prepared using the thin film hydration method and characterized by particle size (PS), zeta potential (ZP), polydispersity index (PDI), % entrapment efficiency (% EE), and % cumulative drug released after 8h (% Q8h ) and 24h (% Q24h). The optimized formulation (SB 5) was incorporated into 1% Carbopol 940 hydrogel (SBG 5) and tested for ex-vivo permeability, skin deposition, and anti-fungal efficacy compared to the commercial formulation (Dermofix® cream) and sertaconazole alone hydrogel (SAG). A randomized controlled clinical trial of SBG 5 compared to Dermofix® cream and SAG was done on 30 patients diagnosed with Tinea corporis with a 4-week follow-up. Results: SB 5 showed PS of 158 ± 6.4nm, ZP of −55 ± 1.7mV, PDI of 0.16 ± 0.01, % EE of 96 ± 3.4, % Q8h of 70.3 ± 3.6, and % Q24h of 97.2 ± 3.0. SBG 5 exhibited in vitro release after 24h (1.25 and 1.51-fold), skin permeability (1.6 and 2.3-fold), skin deposition (3.86 and 14.82-fold), and anti-fungal efficacy against Candida albicans (two and 1.44-fold) compared to Dermofix® cream and SAG respectively. Patients receiving SBG 5 exhibited a 1.25 and 1.8-fold higher recovery rate on days 14 and 21 respectively compared to Dermofix® cream, and a 4.5 and two-fold recovery rate on days 14 and 21 respectively compared to SAG. Conclusion: Bilosomes could be utilized to enhance permeability, skin deposition, anti-fungal properties, and clinical efficacy of Sertaconazole.

Niosome-Based Hydrogel of Quince Extract: A Promising Strategy for Expedited Full-thickness Wound Healing in Rat.

The regeneration of tissue damage involves a series of molecular and cellular events that can be mediated by various natural compounds. Recent studies have highlighted the anti-inflammatory, anti-ulcer, and skin-protecting properties of Cydonia oblonga (Quince), which are mainly attributed to phenolic compounds. These compounds may have some drawbacks when targeting wound applications, including low bioavailability at the wound site. Moreover, to overcome these limitations, surfactant-based nanovesicular systems have been developed as carriers of such compounds for wound healing. This study aimed to highlight the possible therapeutic potential of niosome-based hydrogel from Quince extract to stabilize and deliver the related bioactive compounds to full-thickness wounds in rats. The niosomal hydrogel was prepared using a thin-film hydration method with the fruit extract (70% methanol). The formulation was optimized by evaluating size, zeta potential, dispersion index, and drug encapsulation efficiency. Full-thickness wounds were created on the dorsal cervical area of Wistar rats, and histopathological analysis of biopsy specimens was conducted on the 12th day of treatment. Under the study conditions, niosomal hydrogel displayed good physicochemical stability. Histopathological findings demonstrated that niosomal gel promoted angiogenesis, fibroblast maturation, collagen deposition, keratinization, and epidermal layer formation more effectively than control and hydrogel base. Furthermore, niosomal gel treatment markedly reduced inflammation. The total phenol concentration was determined to be 13.34 ± 0.90 mg gallic acid equivalents per gram of dried extract. The niosomal hydrogel containing C. oblonga extract shows potential as a novel approach for wound healing, warranting further investigation in this field.

Crisaborole-Enthused Glycerosomal Gel for an Augmented Skin Permeation.

Crisaborole (CB), a boron-based compound, is the first topical PDE4 inhibitor to be approved by the US Food and Drug Administration (2016) for the treatment of Atopic Dermatitis. It is marketed as a 2% ointment (Eucrisa, Pfizer). However, CB is insoluble in water; therfore, CB glycersomes were formulated to enhance its permeation flux across the skin. We developed a glycerosomal gel of CB and compared its in vitro release and permeation flux with the 2% conventional ointment. Glycerosomes were prepared using thin film hydration method employing CB, soya phosphatidylcholine, and cholesterol. The formed film was further hydrated employing a mixture of phosphate buffer pH 7.4 /glycerin solution containing varying percentages (20,30, 40, and 50 %) of glycerol. The glycerosomes obtained were characterized by their size, polydispersity index (PDI), and Zeta potential. The entrapment efficiency of the optimized formulation (F1) was determined. The in vitro release of F1 was compared with its 2% conventional ointment. F1 was further incorporated into carbopol 934 P gel. The gel was characterized by pH, viscosity, spreadability, and drug content. The permeability flux of the glycerosomal gel was compared with its 2% conventional ointment. The optimized CB glycerosomes had a vesicle size of 137.5 ± 50.58 nm, PDI 0.342, and zeta potential -65.4 ± 6.75 mV. CB glycerosomal gel demonstrated a 2.13-fold enhancement in the permeation flux. It can thereby be concluded that glycerosomes can be an effective delivery system to enhance the penetration of CB across the skin.

Studying the Characteristics of Curcumin-Loaded Liposomal Nanoparticles

Overview: In this study, the physical and chemical properties of curcumin are extensively examined when it is incorporated into liposome nanoparticles, to enhance its therapeutic potency and bioavailability. Curcumin, a plant-derived polyphenol, has garnered attention for its anti-inflammatory, antioxidant, and anti-cancer activities. However, its clinical utility is hindered by several limitations, including poor water solubility, inadequate absorption, and rapid metabolism. By leveraging the potential of liposome nanoparticles to improve drug delivery and efficacy, this research aims to overcome these obstacles and unlock the full therapeutic potential of curcumin. Methods: Curcumin-loaded liposome nanoparticles (CLLNs) were fabricated employing a thin-film hydration method, after sonication. The physicochemical attributes of CLLNs were subsequently characterized, encompassing particle size and zeta potential assessment utilizing dynamic light scattering (DLS), encapsulation efficiency (EE%) and drug loading efficiency (DLE%) determination through high-performance liquid chromatography (HPLC), investigation of in vitro drug release patterns in simulated biological fluids. Results: The CLLNs optimized in this study had a mean particle diameter of less than 250 nm and a negative surface charge, implying good stability and potential for cellular uptake. The encapsulation efficiency and drug loading efficiency were both found to be high, indicating that curcumin was effectively loaded into the liposomes. In vitro release testing showed a sustained release pattern of curcumin from the CLLNs. Conclusion: The research offered important observations about the advantageous physicochemical features of curcumin-loaded liposome nanoparticles, highlighting their potential as a cutting-edge delivery system for curcumin. The study demonstrated that CLLNs have high encapsulation and drug loading efficiencies, as well as controlled release and improved stability, which suggests their ability to enhance the therapeutic benefits of curcumin. These findings set the stage for future in vivo and clinical trials to fully investigate the potential of CLLNs in medical applications.

Simvastatin-Encapsulated Topical Liposomal Gel for Augmented Wound Healing: Optimization Using the Box-Behnken Model, Evaluations, and In Vivo Studies.

Statins function beyond regulating cholesterol and, when administered systemically, can promote wound healing. However, studies have yet to explore the topical use of statins for wound healing. The present study demonstrated the topical administration of SIM and aimed to formulate, evaluate, and optimize Simvastatin (SIM)-encapsulated liposome gel carrier systems to facilitate successful topical wound healing. Liposomes containing SIM were formulated and optimized via a response surface methodology (RSM) using the thin-film hydration method. The effects of formulation variables, including the 1,2-dioleoyloxy-3-trimethylammoniumpropan (DOTAP) concentration, Span 80 concentration, and cholesterol concentration, on zeta potential (mV), entrapment efficacy (%), and particle size (nm) were studied. The optimized liposome formulation (F-07) exhibited a zeta potential value of 16.56 ± 2.51 mV, revealing robust stability and a high SIM encapsulation efficiency of 95.6 ± 4.2%, whereas its particle size of 190.3 ± 3.3 nm confirmed its stability and structural integrity. The optimized liposome gel demonstrated pseudoplastic flow behavior. This property is advantageous in topical drug delivery systems because of its ease of application, improved spreadability, and enhanced penetration, demonstrating prolonged SIM release. The assessment of the wound healing efficacy of the optimized liposomal gel formulation demonstrated a substantial decrease in wound size in mice on the sixteenth day post-wounding. These findings suggest that the use of liposomal gels is a potential drug delivery strategy for incorporating SIM, thereby augmenting its effectiveness in promoting wound healing.