{"title":"Solid Lipid Nanoparticles as an Innovative Lipidic Drug Delivery System.","authors":"Suchita Waghmare, Rohini Palekar, Lata Potey, Pramod Khedekar, Prafulla Sabale, Vidya Sabale","doi":"10.2174/0122117385271393231117063750","DOIUrl":"10.2174/0122117385271393231117063750","url":null,"abstract":"<p><p>In order to overcome some of the drawbacks of traditional formulations, increasing emphasis has recently been paid to lipid-based drug delivery systems. Solid lipid nanoparticles (SLNs) are promising delivery methods, and they hold promise because of their simplicity in production, capacity to scale up, biocompatibility, and biodegradability of formulation components. Other benefits could be connected to a particular route of administration or the makeup of the ingredients being placed into these delivery systems. This article aims to review the significance of solid lipid nanocarriers, their benefits and drawbacks, as well as their types, compositions, methods of preparation, mechanisms of drug release, characterization, routes of administration, and applications in a variety of delivery systems with a focus on their efficacy.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"22-40"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139692585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development and Characterization of Sulfasalazine Cubosomes for Potential Transdermal Drug Delivery.","authors":"Mekha Mathew, Anasuya Patil, Hemanth G","doi":"10.2174/0122117385269522231113041029","DOIUrl":"10.2174/0122117385269522231113041029","url":null,"abstract":"<p><strong>Background: </strong>Rheumatoid arthritis is indeed a constant, progressive autoimmune disease that acts on the synovial membrane, distinguished by joint pain, swelling, and tenderness. Sulfasalazine belongs to BCS Class IV having low solubility and low permeability. To overcome the issue and provide a localized effect Cubosomes were chosen for the transdermal drug delivery system.</p><p><strong>Objectives: </strong>The primary objective of this investigation was to pass on sulfasalazine-loaded cubosomes over the skin to treat rheumatoid arthritis. On the way to overcome this issue of oral sulfasalazine and provide localized effect, Cubosomes were chosen for the transdermal drug delivery system.</p><p><strong>Methods: </strong>Sulfasalazine-loaded cubosomes were prepared by the top-down method using GMO and Poloxamer 407. Different concentrations of lipid and surfactant were used in the formulation using 3<sup>2</sup> full factorial designs. The prepared formulations were assessed for p.s, z,p, %EE, FTIR, SEM, <i>in-vitro</i> release, <i>ex-vivo</i> permeation, and deposition studies with pH 7.4 phosphate buffer saline.</p><p><strong>Results: </strong>The particle size varies between 65 nm to 129 nm, while the negative zeta potential ranged from - 18.8 mV to -24.8 mV. The entrapment efficiency was between 87% and 95%. The formulations' in-vitro drug release was carried out for 12 hours. The optimized formulation showed a controlled release of sulfasalazine and better ex-vivo permeation and deposition properties than sulfasalazine suspension.</p><p><strong>Conclusion: </strong>Overall study findings support the possibility of applying transdermal sulfasalazineloaded cubosomes to alleviate rheumatoid arthritis.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"320-327"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11851143/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139741682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Devesh U Kapoor, Deepak Sharma, Mansi Gaur, Bhupendra G Prajapati, Sontaya Limmatvapirat, Pornsak Sriamornsak
{"title":"Overcoming Solubility Challenges: Self-emulsifying Systems for Enhancing the Delivery of Poorly Water-Soluble Antiviral Drugs.","authors":"Devesh U Kapoor, Deepak Sharma, Mansi Gaur, Bhupendra G Prajapati, Sontaya Limmatvapirat, Pornsak Sriamornsak","doi":"10.2174/0122117385280541231130055458","DOIUrl":"10.2174/0122117385280541231130055458","url":null,"abstract":"<p><p>The primary goal of drug formulation is to improve a drug's bioavailability in the body. However, poorly water-soluble drugs present challenging issues related to their solubility and bioavailability factors. Emerging technologies, such as lipid-based drug delivery systems, including micro- or nanoemulsifying drug delivery systems, have become increasingly relevant to address the above challenges. This review presents a thorough overview of self-emulsifying drug delivery systems (SEDDS). It covers the properties, principles, self-emulsification mechanism, formulation strategies, and characterization methods of SEDDS. This review also addresses the delivery of antiviral agents through SEDDS. Moreover, it summarizes the marketed formulations of SEDDS consisting of antiviral agents. This review offers a comprehensive and valuable resource for future perspectives on SEDDS and their potential applications in antiviral drug delivery.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"117-132"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139403933","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mohamed S Mansour, Amira A Mahmoud, Mohannad A Sayah, Zahraa N Mohamed, Mohammed A Hussein, Diana A ALsherif
{"title":"RES-CMCNPs Enhance Antioxidant, Proinflammatory, and Sensitivity of Tumor Solids to γ-irradiation in EAC-Bearing Mice.","authors":"Mohamed S Mansour, Amira A Mahmoud, Mohannad A Sayah, Zahraa N Mohamed, Mohammed A Hussein, Diana A ALsherif","doi":"10.2174/0122117385290497240324190453","DOIUrl":"10.2174/0122117385290497240324190453","url":null,"abstract":"<p><strong>Objectives: </strong>Resveratrol (Res) is a bifunctional compound found in numerous plants, including grapes and mulberries. Nanotechnology has promising applications in medicine. The ability of various nanomaterials to serve as radiosensitizers against tumor cells were reported in several manuscripts. The present investigation aimed to assess the antitumor and radiosensitizing effects of Res-CMCNPs on EAC-bearing mice.</p><p><strong>Methods: </strong>Res-CMCNPs have been developed using the CMC emulsification cross-linking technique. Entrapment efficiency (%), particle size, Polydispersity index and ZETA potential, UV, FTIR spectra, and drug release were evaluated and described for RES-CMCNPs. The radiosensitizing properties of RES-CMCNPs were also evaluated <i>in vitro</i> and <i>in vivo</i> against EAC-carrying rodents. The LD50 of Res-CMCNPs was estimated and its 1/20 LD50 was prepared for treating EAC transplanted mice.</p><p><strong>Results: </strong>The results revealed that the Res-CMCNPs exhibited a high entrapment efficiency (85.46%) and a size of approximately 184.60 ±17.36 nm with zeta potential value equals -51.866 mv. Also, the UV spectra of Res and Res-CMCNPs have strong absorption at 225 and 290 nm. The percentage of resveratrol release at pHs 5.8 and 7.4 was found to be 56.73% and 51.60%, respectively, after 24 h at 100 rpm. Also, the FTIR analysis confirmed the chemical stability of resveratrol in Res-CMCNPs cross-linking. The IC<sub>50</sub> values of Res-CMCNPs against EAC cells viability were 32.99, 25.46, and 22.21 μg after 24-, 48- and 72 h incubation, respectively, whereas those of Res- CMCNPs in combination with γ-irradiation after 6-, 10 and 12-mins exposure were 24.07, 16.06 and 7.48 μg, respectively. Also, the LD50 of Res-CMCNPs was 2180 mg/kg.b.w. The treatment of EAC-bearing mice with Res-CMCNPs plus γ-irradiation improved plasma levels of NO, caspase-3, P53 and NF-kB levels as well as liver MDA, GSH, SOD, CAT, LT-B4, aromatase, Bax, Bcl2 and TGF-β levels and exhibited more significant anticancer activity than administration of Res- CMCNPs and/or exposure to γ-irradiation individually. On the other hand, administration of Res- CMCNPs in combination with γ-irradiation attenuated liver mRNAs (21, 29b, 181a, and 451) gene expression.</p><p><strong>Conclusion: </strong>Grafting resveratrol onto carboxymethyl chitosan appears to be a promising strategy for cancer therapy as a radiosensitizer, potentiating tumor cells' sensitivity to radiation by improving levels of proinflammatory features and antioxidant biomarkers.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"254-269"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140859224","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Optimizing Intranasal Amisulpride Loaded Nanostructured Lipid Carriers: Formulation, Development, and Characterization Parameters.","authors":"Manar Adnan Tamer, Hanan Jalal Kassab","doi":"10.2174/0122117385301604240226111533","DOIUrl":"https://doi.org/10.2174/0122117385301604240226111533","url":null,"abstract":"<p><strong>Background: </strong>Nanostructured lipid carriers (NLCs) are lipid-based nanoparticles composed of a mixture of solid and liquid lipids, which are stabilized by the outer surface of a surfactant.</p><p><strong>Objectives: </strong>This research aimed to prepare intranasal nanostructured lipid carriers loaded with amisulpride to enhance its dissolution and bioavailability using different formulation compositions.</p><p><strong>Methods: </strong>Amisulpride nanostructured lipid carriers were formulated using ultra-sonication methods. Solid lipids like stearic acid, palmitic acid, and glyceryl monostearate were used, while liquid lipids like oleic acid, Imwitor 988, and isopropyl myristate were employed. Surfactants used were cremophor®EL, tween 80, and span 20 with different co-surfactants: Transcutol HP, triacetin, and propylene glycol in different ratios. The key metrics used in this study's evaluation were particle size, polydispersity index, zeta potential, entrapment efficiency, and loading efficiency. The formulations with the best characteristics were also subjected to an <i>in-vitro</i> release test.</p><p><strong>Results: </strong>The results showed a significant shift in some evaluation criteria with a non-significant change in other characterizations upon switching between different types and ratios of compositions. A biphasic release pattern was also observed. The optimum formula F19 was found to have 68.309±0.38 nm, 0.2408±0.004, -20.64±0.11 mV, 95.75±0.26 and 18.07±0.36, respectively. It was safe on the sheep nasal membrane.</p><p><strong>Conclusion: </strong>The right combination of the formulation compositions based on studying the effect of each factor on the main formulation characteristics can serve as the basis for a successful intranasal amisulpride-loaded nanostructured lipid carrier.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":"13 2","pages":"287-302"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503222","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Idha Kusumawati, Kresma Oky Kurniawan, Rohmania Rohmania, Bernasdito Ade Pratama, Yusuf Alif Pratama, Subhan Rullyansyah, Mega Ferdina Warsito, Retno Widyowati, Eka Pramyrtha Hestianah, Katsuyoshi Matsunami
{"title":"Comparative Study of Liposomal and Ethosomal Formulations of <i>Curcuma heyneana</i> Rhizome Extract in a Transdermal Delivery System.","authors":"Idha Kusumawati, Kresma Oky Kurniawan, Rohmania Rohmania, Bernasdito Ade Pratama, Yusuf Alif Pratama, Subhan Rullyansyah, Mega Ferdina Warsito, Retno Widyowati, Eka Pramyrtha Hestianah, Katsuyoshi Matsunami","doi":"10.2174/0122117385252518231018161755","DOIUrl":"10.2174/0122117385252518231018161755","url":null,"abstract":"<p><strong>Aims: </strong>This study aimed to develop an anti-aging nanoformulation with <i>Curcuma heyneana</i> extract as bioactive substance.</p><p><strong>Background: </strong><i>Curcuma heyneana</i> Valeton & Zipj extract has been proven in previous research to have antioxidant, anti-ageing, anti-inflammatory, and wound healing properties, which makes it a potential bioactive material for anti-ageing and sunscreen cosmetic products. Phytoantioxidants need to penetrate into deeper skin layers to ensure effectivity. Thus, a transdermal delivery system is needed to deliver the extract to a deeper skin layer.</p><p><strong>Objectives: </strong>The objective of the study was to compare the permeability and anti-ageing activity of liposomal and ethosomal formulations of C. heynena rhizome ethanolic extract.</p><p><strong>Methods: </strong>In this study, <i>C. heyneana</i> extract was loaded into a phospholipid vesicular system in the form of liposome and ethosome formulations using the ethanolic injection method. The anti-ageing activity was assessed by analyzing the epidermal thickness, number of sunburn cells, distance between collagen fibers, and number of fibroblasts. While the histologic specimen scoring was carried out for the in vivo penetration study.</p><p><strong>Results: </strong>The ethosomal formulation had been found to have better penetration ability since it was able to reach the lower dermis area compared to the liposomes, which only reached the upper dermis. The ethosomal formulation of <i>C. heyneana</i> extract exhibited a better anti-ageing activity based on the parameters of epidermal thickness, sunburn cell count, fibroblast count, and the distance between collagen fibres in rat skin histology.</p><p><strong>Conclusion: </strong>Ethosomes have been found to be a more proficient carrier system for transdermal delivery of <i>C. heyneana</i> extract compared to liposomes. Meanwhile, their penetration correlated with the effectivity of the formulation, suggesting that the vesicular system enhanced the penetration ability of the extract.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"303-312"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71484671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel.","authors":"Saba Abdulhadi Jabir, Nawal A Rajab","doi":"10.2174/0122117385285009231222072303","DOIUrl":"10.2174/0122117385285009231222072303","url":null,"abstract":"<p><strong>Background: </strong>Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.</p><p><strong>Objectives: </strong>This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased <i>in situ</i> gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) <i>via</i> using rabbits.</p><p><strong>Methods: </strong>Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive <i>in situ</i> gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (<i>in vitro</i>) and the nasal permeation (<i>ex vivo</i>) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics <i>in vivo</i> studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by Kumar et al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt<sub>0-∞</sub>) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5.</p><p><strong>Results: </strong>The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589 ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p < 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"239-253"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139087984","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Filia Natania, Iriawati Iriawati, Fitria Dwi Ayuningtyas, Anggraini Barlian
{"title":"Potential of Plant-derived Exosome-like Nanoparticles from <i>Physalis peruviana</i> Fruit for Human Dermal Fibroblast Regeneration and Remodeling.","authors":"Filia Natania, Iriawati Iriawati, Fitria Dwi Ayuningtyas, Anggraini Barlian","doi":"10.2174/0122117385281838240105110106","DOIUrl":"10.2174/0122117385281838240105110106","url":null,"abstract":"<p><strong>Aims: </strong>This research aimed to study the potential of PDEN from P. peruviana fruits (PENC) for regenerating and remodeling HDF.</p><p><strong>Background: </strong>Large wounds are dangerous and require prompt and effective healing. Various efforts have been undertaken, but have been somewhat ineffective. Plant-derived exosome-like nanoparticles (PDEN) are easily sampled, relatively cost-effective, exhibit high yields, and are nonimmunogenic.</p><p><strong>Objectives: </strong>The objective of the study was to isolate and characterize PDEN from Physalis peruviana (PENC), and determine PENC's internalization and toxicity on HDF cells, PENC's ability to regenerate HDF (proliferation and migration), and PENC ability's to remodel HDF (collagen I and MMP-1 production).</p><p><strong>Methods: </strong>PENC was isolated using gradual filtration and centrifugation, followed by sedimentation using PEG6000. Characterization was done using a particle size analyzer, zeta potential analyzer, TEM, and BCA assay. Internalization was done using PKH67 staining. Toxicity and proliferation assays were conducted using MTT assay; meanwhile, migration assay was carried out by employing the scratch assay. Collagen I production was performed using immunocytochemistry and MMP-1 production was conducted using ELISA.</p><p><strong>Results: </strong>MTT assay showed a PENC concentration of 2.5 until 500 μg/mL and being non-toxic to cells. PENC has been found to induce cell proliferation in 1, 3, 5, and 7 days. PENC at a concentration of 2.5, 5, and 7.5 μg/mL, also accelerated HDF migration using the scratch assay in two days. In remodeling, PENC upregulated collagen-1 expression from day 7 to 14 compared to control. MMP-1 declined from day 2 to 7 in every PENC concentration and increased on day 14. Overall, PENC at concentrations of 2.5, 5, and 7.5 μg/mL induced HDF proliferation and migration, upregulated collagen I production, and decreased MMP-1 levels.</p><p><strong>Conclusion: </strong>Isolated PENC was 190-220 nm in size, circular, covered with membrane, and its zeta potential was -6.7 mV; it could also be stored at 4°C for up to 2 weeks in aqua bidest. Protein concentration ranged between 170-1,395 μg/mL. Using PKH67, PENC could enter HDF within 6 hours. PENC was non-toxic up to a concentration of 500 μg/mL. Using MTT and scratch assay, PENC was found to elevate HDF proliferation and migration, and reorganize actin. Using immunocytochemistry, collagen I was upregulated by PENC, whereas MMP-1 concentration was reduced.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"358-371"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139513296","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Nanostructured Lipid Carrier-loaded <i>In Situ</i> Gel for Ophthalmic Drug Delivery: Preparation and <i>In Vitro</i> Characterization Studies.","authors":"Vidya Sabale, Vaishnavi Belokar, Manasi Jiwankar, Prafulla Sabale","doi":"10.2174/0122117385266639231029192409","DOIUrl":"10.2174/0122117385266639231029192409","url":null,"abstract":"<p><strong>Background: </strong>Nanostructured lipid carriers (NLCs) are explored as vehicles for ophthalmic drug delivery owing to their better drug loading, good permeation, and satisfactory safety profile.</p><p><strong>Objectives: </strong>The purpose of the study was to fabricate and characterize an <i>in situ</i> ocular gel of loratadine as a model drug based on NLCs to enhance the drug residence time.</p><p><strong>Methods: </strong>NLCs were fabricated using the microemulsion method in which solid lipid as Compritol 888 ATO, lipid as oleic acid, surfactant as Tween 80, and isopropyl alcohol as co-surfactant as alcohol were used. Based on the evaluation of formulation batches of NLCs, the optimized batch was selected and further utilized for the formulation of <i>in situ gel</i> containing Carbopol 934 and HPMC K15M as gelling agents, and characterized Results: The optimized NLCs of loratadine exhibited entrapment efficiency of 83.13 ± 0.13% and an average particle size of 18.98 ± 1.22 nm. Drug content and drug release were found to be 98.67 and 92.48%, respectively. Excellent rheology and mucoadhesion were demonstrated by the loratadine NLC-loaded <i>in situ gel</i> to enhance its attachment to the mucosa. NLC-based <i>in situ</i> ocular gel showed the desired results for topical administration. The prepared gel was observed to be non-irritating to the eye.</p><p><strong>Conclusion: </strong>The optimized NLC-based <i>in situ </i>gel formulation presented better corneal retention and it was found to be stable, offering sustained release of the drug. Thus, the joined system of sol-gel was found promising for ophthalmic drug delivery.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"171-183"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139425225","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}