Drug Permeation Studies Research Articles

Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity.

The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (p < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (p < 0.05) enhanced antifungal activity against C. albicans and A. niger. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery.

Formulation And Evaluation Of Metronidazole Benzoate Loaded Proniosomes For Topical Delivery

In the modern times, vesicular system is a well-known carrier for delivery of drugs. They can carry both lipophilic and hydrophilic drugs. Proniosomes are a vital member of novel drug delivery carriers. The present study was aimed to develop and prepare Metronidazole Benzoate loaded proniosomes with different ratios of cholesterol and non-ionic surfactants to prolong the drug release on topical administration. By slurry method, about fourteen formulations were prepared and evaluated for angle of repose, drug content, particle size, hydration rate, encapsulation efficiency, in-vitro release studies &amp; ex-vivo drug permeation studies. The optimized formulation of proniosomes was developed into transdermal patch and was subjected to various evaluation studies. The in-vitro kinetic and diffusion study of the patch showed a release of 80.71% over 12hrs and fitted into zero order and non-fickian diffusion mechanism. It was summed up, that the formulation F12 containing surfactant: cholesterol as 1:1 was the best formulation. Incorporation into proniosomes can lead to reduced dose, improved bioavailability and prolonged release. Further formulating in form of transdermal patch allows controlled release of the drug. UV spectrophotometric method was developed for determining Metronidazole benzoate in 5% ethanol at 309nm. A regression coefficient value of 0.9977 was noticed. The SEM image as well as the FT-IR spectrum of the optimized formulation was taken to support the same. Hence, we conclude that the proniosomal formulation is a vital candidate for transdermal delivery of metronidazole benzoate in the treatment of various systemic as well as topical bacterial infections.

Applicability of RPMI 2650 and Calu-3 Cell Models for Evaluation of Nasal Formulations.

The RPMI 2650 and Calu-3 cell lines have been previously evaluated as models of the nasal and airway epithelial barrier, and they have demonstrated the potential to be used in drug permeation studies. However, limited data exist on the utilization of these two cell models for the assessment of nasal formulations. In our study, we tested these cell lines for the evaluation of in vitro permeation of intranasally administered drugs having a local and systemic effect from different solution- and suspension-based formulations to observe how the effects of formulations reflect on the measured in vitro drug permeability. Both models were shown to be sufficiently discriminative and able to reveal the effect of formulation compositions on drug permeability, as they demonstrated differences in the in vitro drug permeation comparable to the in vivo bioavailability. Good correlation with the available bioavailability data was also established for a limited number of drugs formulated as intranasal solutions. The investigated cell lines can be applied to the evaluation of in vitro permeation of intranasally administered drugs with a local and systemic effect from solution- and suspension-based formulations.

Fast-Dissolving Nifedipine and Atorvastatin Calcium Electrospun Nanofibers as a Potential Buccal Delivery System.

Geriatric patients are more likely to suffer from multiple chronic diseases that require using several drugs, which are commonly ingested. However, to enhance geriatric patients’ convenience, the electrospun nanofiber system was previously proven to be a successful alternative for the existing oral dosage forms, i.e., tablets and capsules. These nanofibers prepared either as single- or multi-layered fibers could hold at least one active compound in each layer. They might also be fabricated as ultra-disintegrated fibrous films for oral cavity administration, i.e., buccal or sublingual, to improve the bioavailability and intake of the administered drugs. Therefore, in this work, a combination of nifedipine and atorvastatin calcium, which are frequently prescribed for hypertension and hyperlipidemia patients, respectively, was prepared in a coaxial electrospinning system for buccal administration. Scanning electron microscopy image showed the successful preparation of smooth, non-beaded, and non-porous surfaces of the drug-loaded nanofibers with an average fiber diameter of 968 ± 198 nm. In contrast, transmission electron microscopy distinguished the inner and outer layers of those nanofibers. The disintegration of the drug-loaded nanofibers was ≤12 s, allowing the rapid release of nifedipine and atorvastatin calcium to 61% and 47%, respectively, after 10 min, while a complete drug release was achieved after 120 min. In vitro, a drug permeation study using Franz diffusion showed that the permeation of both drugs from the core–shell nanofibers was enhanced significantly (p < 0.05) compared to the drugs in a solution form. In conclusion, the development of drug-loaded nanofibers containing nifedipine and atorvastatin calcium can be a potential buccal delivery system.

Formulation And Evaluation Of Metronidazole Benzoate Loaded Proniosomes For Topical Delivery

In the modern times, vesicular system is a well-known carrier for delivery of drugs. They can carry both lipophilic and hydrophilic drugs. Proniosomes are a vital member of novel drug delivery carriers. The present study was aimed to develop and prepare Metronidazole Benzoate loaded proniosomes with different ratios of cholesterol and non-ionic surfactants to prolong the drug release on topical administration. By slurry method, about fourteen formulations were prepared and evaluated for angle of repose, drug content, particle size, hydration rate, encapsulation efficiency, in-vitro release studies &amp; ex-vivo drug permeation studies. The optimized formulation of proniosomes was developed into transdermal patch and was subjected to various evaluation studies. The in-vitro kinetic and diffusion study of the patch showed a release of 80.71% over 12hrs and fitted into zero order and non-fickian diffusion mechanism. It was summed up, that the formulation F12 containing surfactant: cholesterol as 1:1 was the best formulation. Incorporation into proniosomes can lead to reduced dose, improved bioavailability and prolonged release. Further formulating in form of transdermal patch allows controlled release of the drug. UV spectrophotometric method was developed for determining Metronidazole benzoate in 5% ethanol at 309nm. A regression coefficient value of 0.9977 was noticed. The SEM image as well as the FT-IR spectrum of the optimized formulation was taken to support the same. Hence, we conclude that the proniosomal formulation is a vital candidate for transdermal delivery of metronidazole benzoate in the treatment of various systemic as well as topical bacterial infections

Permeation enhancer nanovesicles mediated topical delivery of curcumin for the treatment of hyperpigmentation

The main aim of the present study was to develop curcumin (CUR) loaded permeation enhancer-lipid vesicles for the treatment of hyperpigmentation. Hyperpigmentation is an acquired skin disorder characterized by uneven skin coloration, mainly in the regions of the facial skin, affecting millions of people worldwide. It often occurs in visible areas, hence causing significant negative psychological and social impacts. In the present study, curcumin-loaded permeation enhancer nanovesicles (PE-NVs) were developed by modified ethanol injection method and dimethyl sulfoxide was added as a penetration enhancer. PE-NVs were subjected to various physicochemical characterizations and drug permeation studies across the skin. The PE-NVs were tested for their efficacy in a sunlight-induced hyperpigmented rabbit skin model. Topical application of PE-NVs reduced symptoms of hyperpigmentation as compared with CUR methanolic solution because of higher accumulation because of better permeation into skin layers. Histopathological studies also confirmed the effectiveness of PE-NVs, since they reduced hyperpigmentation-induced lesions. Results confirmed that PE-NVs is a potential drug delivery system for topical administration drugs to treat skin-associated inflammatory disorders.

Development and Characterization of Transdermal patches of Tramadol Hydrochloride: An Approach to Pain Management

Transdermal drug delivery leads direct access to the systemic circulation through the skin which bypass drug from the hepatic first pass metabolism leading to increase bioavailability. Because Tramadol hydrochloride has low bioavailability, it was selected as a model drug. The present study was aimed to develop and characterize transdermal patches of Tramadol hydrochloride by solvent casting method. Two polymers Ethyl cellulose (EC) and Poly vinyl pyrrrolidine (PVP) in different combination or alone were used to form matrix system. Dibutylpthlate and Glycerine were incorporated as plasticizers. All the patches were characterized for parameters like Thickness, Weight variation, Drug content uniformity, Tensile strength, % elongation, folding endurance, moister content, In-vitro drug permeation study etc. Amongst all formulations, formulation F6 had more desirable characteristic &amp; shows 82.82% drug permeation in 10 hr. Release kinetic can be described by Higuchi model with anomalous diffusion as a release mechanism. The Transdermal patch formulated from Ethyl Cellulose (EC) and PVP showed satisfactory physicochemical properties. So, it can be concluded that such a matrix type patches of Ethyl Cellulose (EC) and PVP could be a good carrier in transdermal delivery of Tramadol HCl. FTIR studies showed there were no incompatibilities between drug and other excipients.

FORMULATION AND DEVELOPMENT OF PRONIOSOMAL GEL FOR TOPICAL DELIVERY OF AMPHOTERICIN B

Objective: The present research work of Amphotericin B Proniosomal gel focuses on improving patient compliance by reducing the side effects of conventional intravenous injections and minimizing the problem of physical stability and to localize drug at site of action. Methods: Proniosomal gels are prepared by coacervation phase separation technique using different concentration of non-ionic surfactants (Span and Tween) for uniform vesicle formation, lecithin as permeation enhancer/membrane stabilizer and cholesterol as a vesicle cement providing prolonged release. Prepared gels were evaluated for their viscosity, pH, spreadability, entrapment efficiency, drug content uniformity, extrudability, in vitro drug release, permeability and stability studies. Results: Among the nine formulations, F2 (containing 10 mg drug, 250 mg Span 60, 50 mg Soya lecithin) was found to be promising. Fourier Transform infra-red (FT-IR) spectra studies represented no interaction and physicochemical characteristics were found within the limits. The percentages of drug content and entrapment efficiency were determined to be 95.16%±0.40 and 94.20%±0.20, respectively. In vitro drug release was about 95.72%±0.30. Conclusion: Proniosomal gel could constitute a promising approach for topical delivery of Amphotericin B by encapsulating it in non-ionic surfactant to provide patient compliance with cutaneous fungal infection, which was found to be safe, tolerable and efficacious.

In vitro skin retention and drug permeation study of Tongluo-Qutong rubber plaster by UPLC/UV/MS/MS

Tongluo-Qutong rubber plaster (TQRP), a typical Chinese patent medicine that contains 13 different herbal remedies, is widely used in clinical practice for the treatment of cervical spondylosis and osteoarthritis. However, due to a lack of in vitro transdermal studies, the active ingredients of TQRP have not been fully elucidated. This presents a huge obstacle for quality evaluation, pharmacokinetic studies and clinical safety assessment of TQRP. In this work, a UPLC/UV/MS/MS method was established and validated to evaluate five analytes in TQRP. The validation demonstrated linearity (r > 0.99), specificity (no co-eluting peaks at the retention times of the analytes), and precision (RSD < 15%) within acceptable parameters. A skin permeation study was performed to determine the concentrations of drugs delivered to the dermis. The 24-hour cumulative permeation of ferulic acid, aleo-emodin, emodin and piperine were 303.68, 709.31, 671.06 and 25561.01 ng/cm2, respectively. According to the fitting data of the TQRP active components, skin permeation was mainly due to a combination of passive diffusion and drug release after matrix erosion.

Design and Development of Mupirocin Nanofibers as Medicated Textiles for Treatment of Wound Infection in Secondary Burns

The present study assessed the topical potential of nanofibers loaded with Mupirocin (MUP) for the treatment of burns. Nanofibers of MUP were composed of Polyvinyl Pyrrolidone (PVP), Gelatin Type-A, and Ethanol using two methods: Solvent casting and Electrospinning. Nanofibers were characterized for Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), Differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA), Drug Content Studies, in-vitro drug permeation, antibacterial and stability studies. The FT-IR studies showed that the Electrospinning technique had a very good mixing of MUP with the polymer. SEM studies showed that the morphology of electrospinning nanofibers had diameters in the range of 70.41 nm- 406.83 nm. The thermal decomposition studies of optimized Nanofiber (E.S.1) were performed by DSC and TGA study and it was found that the formulation had high stability in high-temperature environments. Permeation studies showed that E.S.1 had the highest percentage amount and controlled release of the drug (90 %) up to 8 has compared to other formulations. Nanofibers prepared through the Electrospinning technique showed better antibacterial activity against Staphylococcus aureus as compared to the Solvent casting nanofibers. This research suggested that MUP loaded nanofibers can be potentially used as a topical drug delivery system for the treatment of burns.

Stereolithography-assisted fabrication of 3D printed polymeric film for topical berberine delivery: in-vitro, ex-vivo and in-vivo investigations.

3D printed polymeric film intended for topical delivery of berberine (BBR) was developed using stereolithography (SLA) to enhance its local concentrations. PEGDMA was utilized as photopolymerizing resin, with PEG 400 as an inert component to facilitate BBR solubilization and permeation. Three batches of topical films were printed by varying resin and PEG 400 compositions. In-vitro physicochemical characterizations of the 3D printed films were performed using several analytical techniques including ex-vivo drug permeation studies. In-vivo skin irritation studies were also conducted to assess the skin irritation potential. Films were 3D printed according to design specifications with minimal variations. Microscopic analysis confirmed 3D architecture, while thermal and X-ray diffraction studies revealed amorphous BBR entrapment. Drug permeation study showed effective ex-vivo diffusion up to 344.32 ± 61.20 µg/cm2 after 24.0 h possessing a higher ratio of PEG 400. In-vivo skin irritation studies have suggested the non-irritant nature of printed films. Results indicated the suitability of SLA 3D printing for topical application in the treatment of skin diseases. The presence of PEG 400 in the printed 3D films facilitated BBR diffusion, resulting in an improved flux in ex-vivo model and non-irritant properties in vivo.

Peroral delivery of risedronate sodium for treatment of osteoporosis

Oral route of administration is considered as most widely accepted route which is a potential site for drug delivery, direct access to systemic circulation and site of action. Bisphosphonates are the class of drugs which have been approved for clinical use in osteoporosis and other bone diseases. Bisphosphonates are very poorly absorbed from the GI tract and have limited bioavailability of less than 1% with adverse gastrointestinal effects in humans. The present work aimed to develop sublingual spray formulation using Risedronate sodium with combination of Pullulan gum and HPMC E5. Formulation of sublingual spray was developed by employing optimization technique. The optimized formulation was selected and evaluated for various pharmaco-technical parameters such as viscosity, spray angle, drug content per actuation, In-vitro drug diffusion study, Ex-vivo permeation study and In-vivo pharmacodynamics study by glucocorticoid induced model in rats. Pharmaco-technical parameter results of optimized formulation showed satisfactory results. Comparative In-vitro drug permeation and ex-vivo permeation studies showed maximum drug release of 85% for optimized formulation incorporated with permeation enhance transcutol. In-vivo pharmacodynamic study showed better efficacy in treatment animals with optimized formulation and thus newly developed risedronate sodium sublingual spray proved to be effective used in treatment of osteoporosis.

Chitosan (Poly-(D) glucosamine) based solid lipid nanoparticles of dexibuprofen for topical delivery: Formulation development and characterizations

Chitosan a poly-(D) glucosamine is a polysaccharide made by treating shrimp and other crustacean shells with the alkali sodium hydroxide. It is a hydrophilic polymer that helps to retain the drug inside the solid lipid nanoparticles (SLN’s) and prolongs the release of drug from the carrier system. The purpose of the study was to formulate Chitosan decorated SLN’s for the topical delivery of dexibuprofen by hot pressure homogenization technique. Blank SLN’s, drug loaded SLN’s and Chitosan decorated SLN’s were prepared. Particle size, zeta potential and PDI were determined. FTIR study was conducted to evaluate the compatibility of excipients with the active drug. Surface morphology of SLN’s was determined by field emission scanning electron microscope. Drug content and entrapment efficiency of SLN’s were determined using indirect method. In vitro release and ex vivo permeation study of SLN’s were carried out using Franz diffusion cell. The droplet size fell into the nano range i.e. 132±7 to 424±2 nm which is effective for topical drug delivery system. The PDI of formulations range from 0.21 to 0.42 which depicts the homogeneity of all the SLN’s formulations. Vibrational analysis indicates that there is no interaction between active drug and excipient used in the formulation. The surface morphology revealed the spherical shape of Chitosan decorated SLN’s. The in vitro release of formulations showed 79.91±1.07 to 89.94±1.8 % drug release. The drug permeation study showed high permeation of drug into the skin. The percent drug permeation ranges from 64.15±0.93 to 71.80±0.88% indicating good permeation of drug across the skin. Overall, SLN’s are an effective carrier for topical delivery of dexibuprofen and thus bypasses side effects associated with oral delivery.

Design and Characterization of Buccal Films of Benzocaine for Mouth Ulcer

Mouth ulcer is very common in recent years, which occurs due to the damage of epithelial tissue and/or lamina propria that finally leads to tissue necrosis. Benzocaine has been used to treat the mouth ulcers due to its excellent local anaesthetic effect that relieves the pain associated with mouth ulcer. Hence an attempt was made to develop and characterize the buccal films of Benzocaine to treat mouth ulcers with an aim of prolonging the drug release and improving the patient convenience. The films were fabricated using the mucoadhesive polymer blend of chitosan and HPMC by solvent casting method and the physico-mechanical, in vitro drug release and ex vivo buccal mucosal permeation characteristics of the films were studied. All fabricated film formulations prepared were smooth and almost opaque, with good flexibility. The weight and thickness of all the formulations were found to be uniform. Drug content in the films ranged from 97–99%, indicating favorable drug loading and uniformity. The inclusion of HPMC, significantly reduced the bioadhesive strength and in vitro mucoadhesion time of chitosan films, although the degree of swelling increased. In vitro drug release and permeation studies in simulated saliva showed a prolonged release for a period of 6 h for all formulations. The formulation with Chitosan: HPMC ratio 1:1, 10% w/w polysorbate 80 and 10% w/w propylene glycol as plasticizers showed the best results which exhibited the cumulative percentage drug release of 87.9 % and the cumulative amount of drug permeation of 7.62mg/cm2 across goat buccal mucosa in 6 h. Drug-excipient interaction studies were carried out using DSC and FT-IR technique; films indicated no chemical interaction between drug and polymers used. Keywords: Benzocaine; mouth ulcer; mucoadhesion; buccal film

Polymer Blended Deproteinized Natural Rubber Reservoirs for Nicotine Transdermal Patches: In vitro Drug Release, Permeation Study, and Stability Test

Polymer Blended Deproteinized Natural Rubber Reservoirs for Nicotine Transdermal Patches: In vitro Drug Release, Permeation Study, and Stability Test

Introducing an Efficient In Vitro Cornea Mimetic Model for Testing Drug Permeability

There is a growing need for novel in vitro corneal models to replace animal-based ex vivo tests in drug permeability studies. In this study, we demonstrated a corneal mimetic that models the stromal and epithelial compartments of the human cornea. Human corneal epithelial cells (HCE-T) were grown on top of a self-supporting porcine collagen-based hydrogel. Cross-sections of the multi-layers were characterized by histological staining and immunocytochemistry of zonula oc-cludens-1 protein (ZO-1) and occludin. Furthermore, water content and bssic elastic properties of the synthetized collagen type I-based hydrogels were measured. The apparent permeability coefficient (Papp) values of a representative set of ophthalmic drugs were measured and correlated to rabbit cornea Papp values found in the literature. A multilayered structure of HCE-T cells and the expression of ZO-1 and occludin in the full thickness of the multilayer were observed. The hydrogel-based corneal model exhibited an excellent correlation to rabbit corneal permeability (r = 0.96), whereas the insert-grown HCE-T multilayer was more permeable and the correlation to the rabbit corneal permeability was lower (r = 0.89). The hydrogel-based human corneal model predicts the rabbit corneal permeability more reliably in comparison to HCE-T cells grown in inserts. This in vitro human corneal model can be successfully employed for drug permeability tests whilst avoiding ethical issues and reducing costs.

EFFECT OF ESSENTIAL OILS ON TRANSDERMAL PERMEATION OF METOPROLOL SUCCINATE

The objective of the present study was to prepare a matrix-type transdermal drug delivery system containing metoprolol succinate and to evaluate the effect of essential oils on transdermal permeation of drug. The solvent evaporation method was employed to fabricate transdermal patches of drug using HPMC K15M and Acrycoat L100 as polymers and polyethylene glycol 400 as a plasticizer. Prepared patches were subjected for evaluation of physical as well as physicochemical properties, moisture characteristics, and ex-vivo drug permeation studies. The results of physical characterization showed uniform casting and good appearance of patches. Satisfactory mechanical strength was revealed in the results of tensile strength and folding endurance. Ex-vivo permeation study indicated enhancing effect of essential oils on drug permeation through the skin. The maximum flux observed was 94 μg/cm2.hr achieved by formulation M3 containing lemongrass oil (20%). The results suggested that lemongrass oil was effective at higher concentration (20%) after 14 hrs of permeation while peppermint oil and eucalyptus oil were effective at low concentration (10%). Release kinetic suggested diffusion-controlled release of drug which followed the Korsmeyer-Peppas model. In conclusion, essential oils can be utilized as a safe and effective alternative for the permeation enhancement of drugs through transdermal delivery.

Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation.

The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

Preparation and Characterization of Mucoadhesive Nanoemulsion containing Piperine for Nasal Drug Delivery System

Piperine a bio active constituent isolated from pepper (Piper nigrum and Piper longum L.) is a naturally occurring alkaloid have validated for several health effects and valuable therapeutic effects. However, its biological applications are limited due to its poor aqueous solubility. This emphasizes on the development of new drug delivery system for piperine to improve its in-vivo bioavailability. The present study reports the development and characterization of mucoadhesive nanoemulsion (MNE) containing piperine. MNE formulations were prepared using titration method and characterized in relation to appearance, globule size, zeta potential, thermodynamic stability testing, Ex-vivo evaluation and in-vitro drug permeation study. The MNE of piperine have small globule size (˂ 150nm) and positive zata potential. The spherical surface was confirmed from TEM. pH of MNE was compatible with nasal administration. In vitro release of MNE system in nasal mucosal membrane demonstrated prompt and effective release with more than 75 % of drug release in 4 h.

Formulation and Optimization of Nano Lipid Based Oral Delivery Systems for Arthritis

Rheumatoid arthritis is an autoimmune disease characterized by chronic synovitis that leads to tissue dysfunction as well as loss of complete function. There are several synthetic NSAIDs, glucocorticoids and biological drugs that are commonly used to treat arthritis. These drugs have severe life-threatening side effects. The use of a bioactive compound (Apigenin) could be an alternative to synthetic conventional delivery systems. It is a poorly water-soluble drug having a wide range of pharmacological activities. It has been reported for potential anti-inflammatory and anti-arthritic activity. In the present study, Apigenin (APG) solid lipid nanoparticles were prepared using the solid lipid (glyceryl mono stearate, GMS), surfactant (d -α-Tocopheryl polyethylene glycol 1000 succinate, TPGS) and sonication time (ST). The optimized APG SLNs showed a particle size of 161.7 nm and encapsulation efficiency of 80.44 ± 4.11%. It was further coated with 0.1% w/v chitosan (APG-CH-SLNs) and showed the particle size, PDI and zeta potential of 185.4 nm, 0.45 + 26.7 mV, respectively. The significant (p &lt; 0.001) enhancement in drug release, permeation and mucoadhesive study was observed after chitosan coating. The antioxidant study results depicted an increase in antioxidant property. Finally, the anti-arthritic biochemical parameters revealed marked changes in the results in comparison to arthritic control animals. From the study, it was concluded that APG-loaded mucoadhesive lipid nanoparticles are an alternative to the synthetic oral delivery systems.