Proniosomal Gel Research Articles

Formulation and evaluation of proniosomes containing lornoxicam

Proniosomes are the new generation provesicular drug delivery system of non-ionic surfactant, lecithin and cholesterol which upon reconstitution get converted into niosomes. The objective of current study was to develop stable and sustain transdermal delivery system for lornoxicam. Lornoxicam-loaded topically applied proniosomal gel was formulated, optimized, and evaluated with the aim to deliver drug transdermally. Lornoxicam-loaded proniosomal gels were prepared that contained Lutrol F68 and lecithin as surfactants, cholesterol as a stabilizer, and minimal amount of ethanol and trace water. The resultant lornoxicam-loaded proniosomal gel were assessed for stability and the proniosomes-derived niosomes were characterized for morphology, size, zeta potential, and entrapment efficiency, which revealed that they were suitable for skin application. The coacervation phase separation technique was used in formulation of lornoxicam proniosomal gel and the gel was further assessed for in vitro permeation of lornoxicam through the freshly excised rat skin and the cumulative permeation amount of lornoxicam from proniosome, all exhibited significant increase as compared to 1.0% lornoxicam-loaded pure gel. The optimized F5 batch had shown maximum entrapment efficiency up to 66.98%. It has shown sustained drug release for more than 24h. The skin permeability of proniosomal gel was found to be 59.73%. The SEM and zeta potential studies showed formation of good and stable vesicles. Thus, proniosomes proved to have better potential for transdermal delivery of lornoxicam over conventional gel formulations.

Design and evaluation of proniosomes as a carrier for ocular delivery of lomefloxacin HCl

The current investigation aims to develop and evaluate novel ocular proniosomal gels of lomefloxacin HCl (LXN); in order to improve its ocular bioavailability for the management of bacterial conjunctivitis. Proniosomes were prepared using different types of nonionic surfactants solely and as mixtures with Span 60. The formed gels were characterized for entrapment efficiency, vesicle size, and in vitro drug release. Only Span 60 was able to form stable LXN-proniosomal gel when used individually while the other surfactants formed gels only in combination with Span 60 at different ratios. The optimum proniosomal gel; P-LXN 7 (Span 60:Tween 60, 9:1) appeared as spherical shaped vesicles having high entrapment efficiency (>80%), appropriate vesicle size (187 nm) as well as controlled drug release over 12 h. Differential scanning calorimetry confirmed the amorphous nature of LXN within the vesicles. Stability study did not show any significant changes in entrapment efficiency or vesicle size after storage for 3 months at 4 °C. P-LXN 7 was found to be safe and suitable for ocular delivery as proven by the irritancy test. The antibacterial activity of P-LXN 7 evaluated using the susceptibility test and topical therapy of induced ocular conjunctivitis confirmed the enhanced antibacterial therapeutic efficacy of the LXN-proniosomal gel compared to the commercially available LXN eye drops.

Development and optimization of boswellic acid-loaded proniosomal gel

Context: Boswellic acids (BAs) are isolated from oleo gum of Boswellia serrata and are mainly used as potential anti-inflammatory, hypolipidemic, immunomodulatory, and antitumor agents. Pharmacokinetic investigations of BAs uncover its poor bioavailability through digestive system thus creates a need for improved therapeutic responses which can possibly be achieved by developing formulations through novel delivery system.Objective: Present study was conducted to design topical BA-loaded proniosomal gel for the management of inflammatory disorders with enhanced bioavailability.Materials and methods: Nonionic surfactant vesicles were prepared using the coacervation phase separation method. A central composite design was employed to statistically optimize formulation variables using Design-Expert software. Three independent variables were evaluated: amount of surfactant (X1), amount of soya lecithin (X2), and amount of cholesterol (X3). The encapsulation efficiency percentage (Y1) and particle size (Y2) were selected as dependent variables.Results and discussion: The optimum formulation (F10) displayed spherical bi-layered vesicles under transmission electron microscopy with optimum particle size of 707.9 nm and high entrapment efficiency as 98.52%. In vitro skin permeation study demonstrated the most sustained release of 84.83 ± 0.153 mg/cm2 in 24 h. Anti-inflammatory activity of the gel showed a significant (p < 0.001) higher percentage inhibition as compared to the marketed gel at the same dose.Conclusion: The present study exhibited that BA-loaded proniosomal gel was better in terms of absorption, bioavailability, and release kinetics.

Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 23 factorial design and in vivo evaluation in rabbits

Context: Proniosomes offer a versatile vesicle drug delivery concept with potential for delivery of drugs via transdermal route.Objectives: To develop proniosomal gel using cremophor RH 40 as non-ionic surfactant containing the antihypertensive drug lacidipine for transdermal delivery so as to avoid its extensive first pass metabolism and to improve its permeation through the skin.Materials and methods: Proniosomes containing 1% lacidipine were prepared by the coacervation phase separation method, characterized, and optimized using a 23 full factorial design to define the optimum conditions to produce proniosomes with high entrapment efficiency, minimal vesicle size, and high-percentage release efficiency. The amount of cholesterol (X1), the amount of soya lecithin (X2), and the amount of cremophor RH 40 (X3) were selected as three independent variables.Results and discussion: The system F4 was found to fulfill the maximum requisite of an optimum system because it had minimum vesicle size, maximum EE, maximum release efficiency, and maximum desirability. The optimized system (F4) was then converted to proniosomal gel using carbopol 940 (1% w/w). In vitro permeation through excised rabbit skin study revealed higher flux (6.48 ± 0.45) for lacidipine from the optimized proniosomal gel when compared with the corresponding emulgel (3.04 ± 0.13) mg/cm2/h. The optimized formulation was evaluated for its bioavailability compared with commercial product. Statistical analysis revealed significant increase in AUC (0 − α) 464.17 ± 113.15 ng h/ml compared with 209.02 ± 47.35 ng h/ml for commercial tablet. Skin irritancy and histopathological investigation of rat skin revealed its safety.Conclusions: Cremophor RH 40 proniosomal gel could be considered as very promising nanocarriers for transdermal delivery of lacidipine.

Terconazole Proniosomal Gels: Effect of Different Formulation Factors, Physicochemical and Microbiological Evaluation

Terconazole Proniosomal Gels: Effect of Different Formulation Factors, Physicochemical and Microbiological Evaluation Abstract As treatment of vaginal fungal infection depends mainly on slow release of the drug and prolonged contact time of the delivery system with the vaginal mucosa, proniosomal gel was used as promising candidate to achieve this target. Terconazole, antifungal drug, proniosomal gels were developed based on span 60 and Brij 76 in different molar ratios (1:1, 1:1.5 and 1:2) relative to cholesterol. Proniosomal formulations were hydrated to form niosomes by incorporating into 1% carbopol gel. Proniosomal gel formulations were evaluated for their Entrapment Efficiency (EE%) and vesicle size. Increasing the molar ratio of cholesterol relative to surfactant has affected both EE and vesicle size of prepared niosomes. Drug release profile from different prepared proniosomal gel formulations in simulated vaginal fluid (SVF) was studied in comparison to the commercial product of terconazole for 24 hours. Depending on the high EE% and in-vitro release profile of formulation SC1.5 (1:1.5 span60: cholesterol), it was selected for further evaluations of stability, mucoadhesion to the vaginal mucosa and inhibition of candidas growth. Results indicated that the selected formula, SC1.5, showed good stability and provided higher mucoadhesion and retention time then the commercial product which resulted in more efficient in-vitro inhibition of candida albicans.

Transdermal delivery of oxybutynin chloride proniosomal gels for the treatment of overactive bladder

Context: Overactive bladder (OAB) is a common problem and anticholinergic drugs are first-line therapy, but they have side effects.Objective: Development of oxybutynin chloride (OC) proniosomal gels and analyses of its efficacy for OAB treatment.Materials and methods: Phase separation coacervation was used to prepare proniosomal gels using various non-ionic surfactants, lipids, soy lecithin and isopropyl alcohol. Gels were characterized with regard to entrapment efficiency (EE), vesicle size, surface morphology (using environmental scanning electron microscopy [E-SEM]), stability, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, in vitro skin permeation, in vivo animal studies and histopathology.Results and discussion: EE was 87–92%, vesicle size was 0.38–5.0 μm, and morphology showed some loosened pores in proniosomes after hydration. ATR-FTIR spectroscopy showed no significant shifts in peaks corresponding to OC and excipients. Most formulations exhibited >50% permeation but the cholesterol-containing formulations P3 (Span 20:Span 60 [1:1]) and P4 [Tween 20:Tween 80 (1:1)] had the highest percent cumulative permeation. P3 and P4 also showed faster recovery of cholinergic effects on salivary glands than oral formulations. P3 and P4 had pronounced therapeutic effects in reduction of urinary frequency and demonstrated improvements in bladder morphology (highly regenerative surface of the transitional epithelium).Conclusion: These results suggest that OC could be incorporated into proniosomal gels for transdermal delivery in the treatment of OAB.

Systematically optimized coenzyme q10-loaded novel proniosomal formulation for treatment of photo-induced aging in mice: characterization, biocompatibility studies, biochemical estimations and anti-aging evaluation

Environmental stress and advancing age is considered as the main cause of skin aging. However, environmental stress (especially UV radiations) accelerates the process of skin aging by manifolds. Coenzyme Q10 (CoQ10), an essential compound of cellular bioenergetics also acts as a strong antioxidant and protects the body against aging. High molecular weight and structure specific lipophilic nature of this molecule is a bottle neck in effective delivery through topical route. Preparation of a novel proniosomal (PN) gel formulation of CoQ10 employing systematic design of experiment (DoE) approach is a step ahead in transcending the constraints of the topical delivery. I-optimal mixture design was employed for systematic optimization of proniosomal formulation and evaluation of experimental data was performed for entrapment efficiency and in vitro release. Hydration of PN gel formulation with phosphate buffer (pH 7.5) results in submicron niosomes vesicles of spherical shape, which appeared dark against bright surroundings in TEM study. Animal skin was treated with UV radiations followed by treatment of PN gel CoQ10 and conventional CoQ10 present in a gel base. The effectiveness of the treatment was evaluated on the basis of biochemical estimation and histopathological studies. By using CoQ10 PN gel formulation, levels of superoxide dismutase (SOD), catalase (CA), glutathione (GSH) and total proteins were restored by 81.3%, 72.1%, 74.8 and 77.1%, respectively to that of control group. Histopathological studies revealed better protection of skin treated with CoQ10 PN gel compared to free CoQ10. Prepared PN gel was found undisturbing with the normal histology hence, tolerated by animal skin compare to conventional gel.

Novel Vesicular Drug Delivery System for Topical Delivery of Indomethacin

The aim of the present research work was to develop and evaluate provesicular topical drug delivery system of indomethacin. The encapsulation of drug in vesicular structure prolongs the existence of the drug in the systemic circulation with improved bioavailability. The potential of proniosomes as a topical drug delivery system was explored by formulating proniosomal gel of indomethacin using coacervation-phase separation method with different ratios of sorbitan fatty acid esters (Span 60) and cholesterol. The formulations were characterized for various parameters like vesicle size and shape, drug entrapment, in vitro drug release profiles and vesicular stability at different storage conditions. In-vitro studies showed slow and sustained release of entrapped indomethacin. Stability studies for optimized proniosomal gel were conducted for 3 months. The current research work demonstrated that proniosomes are stable and promising topical drug delivery system for indomethacin. Keywords: Gel, indomethacin, in-vitro release, proniosomes, stability studies, topical delivery.

Formulation and development of industry feasible proniosomal transdermal drug delivery system of granisetron hydrochloride

Proniosomes gel is semisolid liquid crystal products of nonionic surfactants, which converted into niosomes upon hydration. A proniosome based transdermal drug delivery system of granisetron hydrochloride (GRA HCL) developed by coacervation phase separation method. Formulation optimized by use of 32 full factorial design. Span 60 and cholesterol selected as independent variables, while entrapment efficiency (EE) and flux selected as dependent variables. Proniosomes evaluated for EE, in vitro permeation study, stability study, microscopial examination by photomicroscopy, scanning electron microscopy, particle size analysis. F5 batch containing 90 mg span 60, and 10 mg cholesterol show maximum entrapment (66.57 ± 0.20%) and flux (7.94 ± 0390 μg/cm2/h). Comparative in vitro drug release study of plain drug solution and drug in proniosomal gel form was carried out for 48 h on guinea pig skin. It was found that cumulative release and flux of proniosomal gel was nearly two times more than drug solution containing same drug concentration.The study demonstrated the effectiveness of proniosomal transdermal patch containing GRA HCL for effective management of chemotherapy induced nausea and vomiting. Key words: Factorial design, industry feasible, niosomes, proniosomes, stability, transdermal drug delivery

DESIGN AND EVALUATION OF PRONIOSOMES AS DRUG CARRIER FOR OCULAR DELIVERY OF LEVOFLOXACIN

The objective of present work is to develop proniosomal ocular gel of Levofloxacin and evaluation of their potential for sustained ocular delivery. The conventional liquid ophthalmic formulation is eliminated from the precorneal area immediately upon instillation and it is difficult to achieve good bioavailability of drug due to the tear production, non productive absorption, impermeability of corneal epithelium and transient residence time. As a result, frequent instillation of concentrated solutions is needed in order to achieve the desired therapeutic effects. The bioavailability can be enhanced by the use of vesicular systems such as Niosomes. But, Aqueous suspensions of Niosomes may exhibit aggregation, fusion, leaking of entrapped drug or hydrolysis of encapsulated drug, thus limiting the shelf life of the dispersion. The proniosomal approach minimises the above-mentioned problems and therefore there is ease of transfer, distribution, measuring and storage which makes proniosomes a versatile delivery system. Levofloxacin Proniosomal gel enhances the contact time and retention in the eye and provides sustained release action and better availability of drug.

Oro-dental mucoadhesive proniosomal gel formulation loaded with lornoxicam for management of dental pain

Oro-dental diseases are generally associated with pain that is controlled using oral tablets containing NSAIDs. Lornoxicam, a relatively new NSAID, is effective in relieving pain accompanying different oro-dental problems. The aim of the current research is to prepare oro-dental analgesic and anti-inflammatory gel using provesicular approach to deliver lornoxicam directly to the site of action in the oral cavity. Local administration of lornoxicam is expected to be superior to systemic delivery in pain relieving and poses less GIT adverse effects. Different surfactants were utilized to prepare the proniosomal gels that rapidly transform into nano-sized niosomes after hydration with the oral saliva. The effect of the surfactant structure on vesicles size distribution and entrapment efficiency percentage (EE%) was investigated. The proniosomal formulations were incorporated into carbopol hydrogels that were characterized regarding rheological and mucoadhesion properties. Moreover, ex-vivo mucosal membrane permeation studies were conducted for selected proniosomal gels to quantify the permeation parameters and assess the amount of drug deposited within the oral mucosa. Results revealed that mucoadhesive proniosomes formulation prepared using Span 60 was optimal as it was nano-sized and also showed the highest EE%. The transmucosal flux of lornoxicam, from these proniosomal formulations, across the oral mucosa was significantly higher (p < 0.05) than lornoxicam containing carbopol gel and the percent drug diffused increased more than twofolds. The results collectively suggest that the mucoadhesive proniosomal gels can be assertively considered as a promising carrier for transmucosal delivery of lornoxicam into the oral cavity.

Nano-proniosomes enhancing the transdermal delivery of mefenamic acid

Mefenamic acid (MA) is a BCS II class NSAID drug. It is available only in the form of tablets, capsules, and pediatric suspensions. Oral administration of MA is associated with severe gastrointestinal side effects. The aim of this study was to develop a convenient and low-cost transdermal drug delivery system for MA using proniosome as a novel carrier without the addition of penetration enhancers. The formulation factors, such as the presence of cholesterol, types of lecithin, and surfactants were investigated for their influence on the entrapment efficiency, rate of hydration, vesicle size, and zeta potential, in vitro drug release and skin permeation in order to optimize the proniosomal formulations with the minimum dose of the drug. Furthermore, the in vivo anti-inflammatory effect was evaluated on a formalin-induced rat paw edema model. The results showed that the type of surfactants had higher impact on the entrapment efficiency than the type of lecithins, with the highest in Span 80 (82.84%). The release of MA from Span 80 proniosomal gel was significantly affected by the type of lecithin used. The addition of cholesterol significantly increased both the drug release and the skin permeation flux of MA. Zeta potential showed a stable A4 noisomal suspension. DSC revealed the molecular dispersion of MA into the loaded proniosomes. In vivo study of the treatment group with MA proniosome gel showed a significant inhibition of rat paw edema compared with the same gel without the drug (control). The results of this study suggest that proniosomes are promising nano vesicular carriers and safe alternatives to enhance the transdermal delivery of MA.

An electron spin resonance study of non-ionic surfactant vesicles (niosomes)

Certain non-ionic surfactants form lamellar vesicles called niosomes. Being elastic and deformable, niosomes have been used as an efficient vehicle for transdermal drug delivery. However, dynamic properties of niosomes have not been studied extensively. In this study we used electron spin resonance (ESR) technique to measure the membrane fluidity of niosomes. In parallel with phospholipid liposomes, the ESR spectra of 5- and 16-doxyl stearate in niosomes of sorbitan monostearate (Span 60) and sorbitan monooleate (Span 80) showed that motion of the spin label was more restricted at the region near the headgroup than near the bilayer center. Cholesterol increased fluidity of Span 60 niosomes whereas it decreased fluidity of Span 80 niosomes. Dicetyl phosphate added at 10mol% concentration as a stabilizer had a minimal effect on the membrane fluidity throughout the bilayer. We also used ESR technique to monitor the hydration-induced transformation of Span 60 proniosome gel to niosome and showed that the niosome prepared by hydration of proniosome gel was identical to the niosome obtained from a thin film hydration method. Finally the ESR spectra of Span niosomes were compared with those of polysorbate (Tween) niosomes and polyethoxy fatty ether (Brij) niosomes. Tween niosomes had a bulky headgroup and were much less rigid than Span niosomes. This effect of headgroup size on fluidity was also manifest in Brij niosomes where fluidity increased with the number of ethoxy units in the polyethoxy headgroup.

FORMULATION AND EVALUATION OF CANDESARTAN CILEXETIL TRANSDERMAL PRONIOSOMAL GEL

The present work deals with the preparation of candesartan cilexetil proniosomal gel by coaservation phase separation method by using different surfactants, cholesterol and soya lecithin in 9:1:9 and 9:2:9 ratios. The prepared proniosomal gel formulations were evaluated for vesicle size analysis, surface morphological studies, encapsulation efficiency, In vitro drug release, ex vivo skin permeation studies and vesicular stability at different storage conditions. The results showed that candesartan cilexetil in all the formulations was successfully entrapped and a substantial change in release rate and an alteration in the encapsulation efficiency of candesartan cilexetil from proniosomes were observed upon varying the type of surfactant and cholesterol content. Vesicles formed with Spans were smaller in size than vesicles formed with Tweens. Encapsulation efficiency of proniosomes formed from Span 60, Span 40, Span20, and Span 80 was found high compared with proniosomes prepared from Tweens (Tween 20 and Tween 80). An optimised preparation with 9:2:9 ratio of Span 60, cholesterol and lecithin gave maximum encapsulation efficiency (92.29%) and showed drug release (95.89±0.26%) in a controlled manner with a flux value of 1.89 μg/cm2 /hr and permeability co efficient value of 0.094 cm2/hr as compared to other compositions. No significant changes in relation to vesicle size and encapsulation efficiency were recorded after stability studies. It is evident from this study that proniosomes are a promising prolonged delivery system for candesartan cilexetil and have reasonably good stability characteristics. Keywords: candesartan cilexetil, proniosomes, encapsulation efficiency, flux, stability.

In vitro Dynamics of Ibuprofen Incorporated Proniosomal Gel

Aim: The research was aimed to encapsulate the ibuprofen with proniosomal gel and facilitate ibuprofen release in sustained manner for sustained drug release. Methods: Different proniosomal gels of ibuprofen were formulated with Span 20/Span 80 and soya lecithin using the method described in literature. In all formulations cholesterol concentration was kept constant. The prepared proniosomal gels were evaluated for chemical incompatibility by FT-IR, vesicle size analysis, encapsulation efficiency, in vitro drug permeation and in vitro drug release kinetics were performed. Results: The principal absorption peaks of ibuprofen were retained in the proniosomal gels indicating that there was no interaction between ibuprofen and excipients. Vesicular diameter markedly depended on the type of the non-ionic surfactant used. As the outer diameter depends on the HLB value of surfactant, the vesicular diameter was less for proniosomes prepared using Span 80 (low HLB). The encapsulation efficiency was more for the proniosomal gels prepared using Span 20. Proniosomal gel prepared using Span 80 showed higher flux across the membrane due to its leaky membrane. The order of ibuprofen release from the proniosomal gel was PN2>PN4>PN1>PN3. Conclusion: The optimized proniosomal gel formulation PN3 containing Span 20 exhibited prolonged ibuprofen release profiles. Fickian diffusion mechanism was observed with the PN3 formulation which was due to the sustained release property. The results indicated that the proniosomal gel would be an effective transdermal delivery system for ibuprofen.

Proniosomes as a novel drug carrier system for buccal delivery of benzocaine

Benzocaine proniosomal gel formulations were prepared using Span 60, Span 80 or Span 85 and their mixtures. Drug entrapment efficiency increased with the increase of the ratio of Span 80 or Span 85 in the surfactant mixture from 8.19 % up to 26.21 %. The addition of Span 80 or Span 85 to Span 60 obviously decreased the vesicle sizes from 825 to 190 nm. The in vitro release pattern of Benzocaine showed an initial fast release followed by a slower release rate. Formulations containing Span 80 and Span 85 showed better rate and extent of Benzocaine permeation when examined using chicken pouch as a model mucosal membrane. Physical stability studies showed a drug retention of > 90 % after storage for 30 days at 4-8 °C. This study shows the potential of using proniosomal benzocaine as an effective, long acting vesicular formulation for improving local anesthesia in the buccal cavity.

Formulation and Evaluation of Proniosome Based Drug Delivery System of the Antifungal Drug Clotrimazole

In the present study proniosomal gel of clotrimazole was formulated by using lecithin, cholesterol as encapsulating agents, nonionic surfactants Span and Tween with different grades. Evaluation of proniosomal gels for pH, vesicle size analysis, encapsulation efficiency, drug diffusion profiles, ex-vivo skin permeation and ex-vivo drug deposition studies on guinea pig skin, irritation test on rabbit and stability studies was performed. The preliminary compatibility studies revealed that there were no interactions between clotrimazole and excipients which was evident from FTIR and DSC studies. The physical characteristics of proniosomal gels were found to be within the acceptable limits. The vesicle size was found to be in the range 5.25-15.23μm. The proniosomes were spherical and homogenous in structure when observed under optical microscopy. The ex-vivo skin permeation and ex-vivo drug deposition studies showed the drug release from formulations F3, F4 and marketed formulation was 48.60%, 36.9% and 27.48 % respectively and the percent of clotrimazole deposited in skin after 24 h was found to be 35.7%, 43.6% and 15.17% for formulation F3, F4 and marketed formulation respectively. The release from the proniosomal gel was prolonged when compared to conventional formulation and showed a two fold increase in the drug deposition in the skin compared to conventional cream. No obvious erythema, edema or inflammation was observed on rabbits’ skin after one week of application of the selected formulation. Results of antifungal studies revealed that the developed proniosomal gel is more efficient when compared with the marketed formulation. The stability studies showed that proniosomal gels were stable at 5±3°C and 25±2°C. The above results indicated that the proniosomal gels of clotrimazole could be formulated for sustained release.

Encapsulation of bio active compound ursolic acid as proniosomes and its evaluation

In the present study, novel proniosomal gel of ursolic acid was prepared by encapsulation of the drug in a mixture of span 60, cholesterol and alcohol by coacervation phase separation method to overcome the bioavailability problem of this potential biologically active compound. The formulated system was characterized for size, drug entrapment, in‑vitro drug release studies and in‑vivo anti‑inflammatory effect through animal model. In‑vitro release data of ursolic acid from proniosomal gel revealed a time dependent near linear relationship. Entrapment efficiency of the formulated gel was found > 90% and total % cumulative release of ursolic acid satisfactory as 60.8% after 24 h. Release pattern was also found almost constant. In‑vivo evaluation revealed that the developed formulation exhibited significant anti‑inflammatory value (P < 0.05) in carrageenan induced rat paw edema model and was found quite comparable with the standard diclofenac gel (voveran gel) in terms of % inhibition of edema. Key words: Non‑steroidal anti‑inflammatory drugs, proniosomes, topical drug delivery, ursolic acid

ENHANCEMENT OF FOLLICULAR DELIVERY OF FINASTERIDE IN NIOSOMALAND PRONIOSOMAL GEL FORM FOR TREATING ANDROGENETIC ALOPECIA

Finasteride has not been explored extensively for the treatment of androgenic alopecia. The present workwas aimed to enhance the follicular delivery of finasteride topically by niosomal and proniosomal carriersystems for treating androgenetic alopecia. Finasteride niosomes were prepared by thin film hydrationmethod and proniosomes were prepared by coacervation phase separation method. The niosomesprepared with cholesterol-Span 20 (1:1) and proniosmes prepared with cholesterol-Span 20 (1:1) showedbetter mean vesicle size, drug content, in vitro release profile and skin permeability. The effect of chargeinducer, dicetyl phosphate (DCP) on skin permeability of niosomes and proniosomes was studied and itwas found to be less in this study. Stability studies were preformed and the formulation was found to bestable for 60 days. Clinical trials by phototrichogram method was performed for proniosomal formulationwith cholesterol-Span 20 (1:1) and DCP on twenty healthy male volunteers and it was found to increasethe anagen hair count of test group by 42.85 % when compared with the control group (6.6%), indicatingthe proniosomal gel formulation achieved the objective of enhancing the drug concentration in androgenicreceptors of hair shaft and thus it can be used safely for treating androgenic alopecia.

PRONIOSOMAL GEL OF FLURBIPROFEN: FORMULATION AND EVALUATION

The purpose of this research is to design proniosomal gel drug delivery system of flurbiprofen in a trial to overcome the adverse effects associated with oral administration of the drug. This can be overcome by the use of vesicular drug delivery system. Encapsulation of a drug in vesicular structure can be predicted to prolong the existence of the drug in the systemic circulation and thus enhance penetration into target tissue and reduce toxicity. Proniosomal gels are generally present in transparent, translucent or white semisolid gel texture. Due to the limited solvent system present, the proniosomes formed were the mixture of many phases of liquid crystal, viz. lamellar, hexagonal and cubic phase liquid crystals. The potential of proniosomes as a transdermal drug delivery system for flurbiprofen was investigated by encapsulating the drug in various formulations of proniosomal gel composed of various ratios of sorbitan fatty acid esters, cholesterol, prepared by coacervation-phase separation method. The formulated systems were characterized in vitro for size, vesicle count, drug entrapment, drug release profiles and vesicular stability at different storage conditions. Stability studies for proniosomal gel were carried out for 4 weeks. The method of proniosome loading resulted in an encapsulation yield of 30.6 – 75.4%. Proniosomes were characterised by transmission electron microscopy. In vitro studies showed prolonged release of entrapped flurbiprofen. At refrigerated conditions, higher drug retention was observed. It is evident from this study that proniosomes are a promising prolonged delivery system for captopril and have reasonably good stability characteristics.